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EMI1 is an EGFR ex19del/T790M/C797S and EGFR L858R/T790M/C797S inhibitor. EMI1 can be used for the research of mutant EGFR-associated, drug-resistant non-small-cell lung cancer (NSCLC) .
CH7233163 is a noncovalent ATP-competitive inhibitor for EGFR-Del19/T790M/C797S. CH7233163 can overcome Osimertinib (HY-15772)-Resistant EGFR-Del19/T790M/C797S mutation. CH7233163 blocks the EGFR phosphorylation in the Del19/T790M/C797S_NIH3T3 cells. CH7233163 has antitumor activities .
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR d746-750/T790M/C797S Recombinant Human Active Protein Kinase is a recombinant EGFR d746-750/T790M/C797S protein that can be used to study EGFR d746-750/T790M/C797S-related functions .
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR T790M/C797S/L858R Recombinant Human Active Protein Kinase is a recombinant EGFR T790M/C797S/L858R protein that can be used to study EGFR T790M/C797S/L858R-related functions .
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR d746-750/T790M/C797S/L858R Recombinant Human Active Protein Kinase is a recombinant EGFR d746-750/T790M/C797S/L858R protein that can be used to study EGFR d746-750/T790M/C797S/L858R-related functions .
EGFR-IN-27 is a potent EGFR inhibitor with IC50s of <50 nM for EGFR Del, L858R, Del/T790M, L858R/T790M, Del/T790M/C797S, and L858R/T790M/C797S, respectively (WO2021249324A1, compound 511) .
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR T790M Recombinant Human Active Protein Kinase is a recombinant EEGFR T790M protein that can be used to study EGFR T790M-related functions .
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR C797S Recombinant Human Active Protein Kinase is a recombinant EGFR C797S protein that can be used to study EGFR C797S-related functions .
EGFR-IN-95 (compound 5j) is an 2,4-diaminonicotinamide derivative. EGFR-IN-95 has potent inhibitory activity against EGFRdel19/T790M/C797S and L858R/T790M/C797S .
EGFR-IN-133 (Compound 24) is an inhibitor for EGFR, that inhibits the EGFR wildtype, L858R/T790M, d19/T790M, L858R/T790M/C797S, and d19/T790M/C797S mutans with IC50 of 0.1, 0.044, 0.036, 0.04, and 0.054 nM. EGFR-IN-133 exhibits good pharmacokinetics characteristics with high oral exposure .
EGFR-IN-132 (Compound 23) is an inhibitor for EGFR, that inhibits the EGFR wildtype, L858R/T790M, d19/T790M, L858R/T790M/C797S, and d19/T790M/C797S mutans with IC50 of 1.6, 0.025, 0.019, 0.022, and 0.029 nM. EGFR-IN-132 exhibits good pharmacokinetics characteristics with high oral exposure .
EGFR-IN-98 (Compound 4c) is a EGFR inhibitor. The IC50 values of L858R/T790M/C797S and Del19/T790M/C797S are 0.277 μM and 0.089 μM, respectively. EGFR-IN 98 can be used in the study of tumors .
EGFR-IN-69 (compound 17g) is a potent EGFR inhibitor, with IC50 values of 4.3, 6.6 and 25.6 nM against EGFR L858R/T790M/C797S, EGFR L858R/T790M, and EGFR 19del/T790M/C797S, respectively. EGFR-IN-69 can be used for non-small-cell-lung-cancer (NSCLC) research .
LS-106 is an orally active and potent inhibitor against epidermal growth factor receptor (EGFR) . LS-106 exhibits antitumor activities both in vitro and in vivo. LS-106 inhibits the kinase activities of EGFR19del/T790M/C797S and EGFRL858R/T790M/C797S with IC50 values of 2.4 nmol/L and 3.1 nmol/L, respectively, which is more potent than Osimertinib (HY-15772). LS-106 induces Apoptosis, suppresses cell proliferation of tumor cells harboring EGFR 19del/T790M/C797S and leas to significant tumor regression in a C797S-mutant xenograft model .
Os30, a potent fourth-generation EGFR inhibitor, is a potent EGFRC797S-TK inhibitor with IC50 values of 18 nM and 113 nM for EGFRDel19/T790M/C797S TK and EGFRL858R/T790M/C797S TK, respectively. Os30 can suppress EGFR phosphorylation, arrest at G1 phase and induce the apoptosis of KC-0116 (BaF3-EGFRDel19/T790M/C797S) cells. Os30 shows potent antitumor efficacy on non-small cell lung cancer (NSCLC) with EGFmRC797S mutation .
EGFR-IN-97 (compound 6q) is a EGFR inhibitor. EGFR-IN-97 shows inhibitory activity against Ba/F3-EGFR L858R/T790M/C797S and Ba/F3-EGFR Del19/T790M/C797S cells, with IC50 values of 0.42 μM and 0.41 μM, respectively. EGFR-IN-97 can promote apoptosis of NCI-H1975-EGFR L858R/T790M/C797S cells at the concentration of 0.8 μM .
EGFR kinase inhibitor 2 (compound A-7) is a potent EGFR inhibitor targeting EGFR L858R/T790M/C797S and EGFR Del19/T790M/C797S mutants. EGFR kinase inhibitor 2 has the potential to address acquired resistance in the treatment of non-small cell lung cancer .
EGFR-IN-140 (Compound 31) is the inhibitor for EGFR, that inhibits EGFR wildtype and EGFR L858R/T790M/C797S mutant with Ki of 0.95 nM and 2.1 nM, and inhibits EGFR del19/T790M/C797S in Ba/F3 with an IC50 of 56.9 nM. EGFR-IN-140 exhibits antitumor efficacy in mouse model .
EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) with an IC50 of 18 nM for triple mutant EGFR L858R/T790M/C797S. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1 .
JND3229 is a reversible EGFR C797S inhibitor with IC50 values of 5.8, 6.8 and 30.5 nM for EGFR L858R/T790M/C797S, EGFR WT and EGFR L858R/T790M, respectively. JND3229 has good anti-proliferative activity and can effectively inhibit tumour growth in vivo. JND3229 can be used in cancer research, especially in non-small cell carcinoma .
EGFR mutant-IN-2 (Compound D51) is an EGFR mutant inhibitor. EGFR mutant-IN-2 inhibits the EGFR L858R/T790M/C797S mutant with an IC50 value of 14 nM. EGFR mutant-IN-2 inhibits the EGFR del19/T790M/C797S mutant with an IC50 value of 62 nM. EGFR mutant-IN-2 has favorable PK parameters, safety properties, in vivo stability, and antitumor activity .
EGFR-IN-101 (I-10) is a 2-phenylamino pyrimidine derivative. EGFR-IN-101 is a EGFR inhibitor. The IC50 values for EGFR L858R/T790M/C797S and Ba/F3-EGFR L858R/T790M/C797S are 33.26 and 106.4 nM, respectively. EGFR-IN-101 can be used IN the study of non-small cell lung cancer (NSCLC) .
EGFR-IN-117 (Compound 8h) exhibits inhibitory activity against EGFR mutation, targets the tumor environment, and induces apoptosis of cancer cells. EGFR-IN-117 inhibits proliferations of H1975, PC-9, and EGFR mutant cells BaF3-EGFR L858R/T790M/C797S and BaF3– C797S/Del19/T790M, with IC50 of 13 nM, 19 nM, 1.2 nM and 1.3 nM, respectively. EGFR-IN-117 exhibits antitumor efficacy in mouse models .
Mutated EGFR-IN-3 (compound 3) is a potent, ATP-competitive and highly selective allosteric dibenzodiazepinone inhibitor of the EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) mutants with IC50 values of 12 nM and 13 nM, respectively .
EGFR-IN-90 (compound 34) is an orally active EGFR inhibitor. EGFR-IN-90 shows inhibitory activity against EGFRL858R/T790M/C797S with an IC50 of 5.1 nM and inhibits the proliferation of the H1975-TM cell line harboring EGFRL858R/T790M/C797S with an IC50 of 0.05 μM. EGFR-IN-90 and inhibits tumor growth in the H1975-TM xenograft tumor model .
EGFR T790M/VEGFR-2-IN-1 (Compound 6) is a dual EGFR T790M mutant (IC50=0.26 μM) and VEGFR-2 (IC50=0.95 μM) inhibitor. EGFR T790M/VEGFR-2-IN-1 blocks tumor cell proliferation and angiogenesis signaling pathways. EGFR T790M/VEGFR-2-IN-1 exhibits potent cytotoxicity against multiple cancer cell lines (HCT116, MCF-7, HepG2, A549; IC50=5.35-9.90 μM). EGFR T790M/VEGFR-2-IN-1 is promising for research of non-small cell lung cancer and solid tumors .
EGFR-IN-82 (Cmpound 8a) is a potent and orally active EGFR inhibitor with IC50 values of 0.09 and 0.06 nM for EGFR L858R/T790M/C797S and EGFR Del19/T790M/C797S, respectively. EGFR-IN-82 has no significant effect on EGFR WT. EGFR-IN-82 has anti-proliferative activity and inhibits tumor formation in nude mice. EGFR-IN-82 can be used in non-small cell lung cancer research .
EGFR-IN-48 is a potent and orally active EGFR inhibitor with IC50s of 0.193 nM, 0.251 nM, 10.4 nM for EGFR d19/TM/CS, EGFR LR/TM/CS, EGFR WT, respectively. EGFR-IN-48 inhibits the proliferation of BaF3 EGFR del19/T790M/C797S and PC-9 EGFR del19/T790M/C797S cells with IC50s of 1.526, 66.7 nM, respectively .
EGFR-IN-104 (Compound A23) is an effective inhibitor of EGFR, with IC50 values of 0.33 μM and 0.133 μM against EGFR L858R/T790M and EGFR Del19/T790M/C797S, respectively. EGFR-IN-104 exhibits anticancer activity both in vitro and in vivo .
HJM-561 is a selective and effective orally active EGFRPROTAC degrader. HJM-561 is able to overcome the triple EGFR mutations that are resistant to Osimertinib (HY-15772). HJM-561 exhibits potent degradation of EGFR Del19/T790M/C797S (DC50: 9.2 nM) and L858R/T790M/C797S (DC50: 5.8 nM), and has anti-tumor activity (pink: EGFR ligand (HY-12857); blue: CRBN ligand (HY-A0003); black: linker) .
EGFR/C797S-IN-1 is a potent EGFR-C797S inhibitor with an IC50 value of 0.128 µM. EGFR/C797S-IN-1 shows anti-proliferative activity and anti-tumor activity. EGFR/C797S-IN-1 inhibits the expression of p-EGFR in a dose-dependent manner .
EGFR WT/T790M-IN-2 (Compound 7c) is a EGFR T790M/WT inhibitor with IC50 values of 0.08 and 0.13 μM, respectively. EGFR WT/T790M-IN-2 induces apoptosis by blocking the G0-G1 phase (apoptosis). EGFR WT/T790M-IN-2 has antitumor activity .
BI-4732 is an orally active, reversible, ATP-competitive EGFR inhibitor with blood-brain barrier penetration. BI-4732 inhibits the kinase activity of EGFR L858R, T790M and C797S with IC50 values of 1 nM while sparing EGFR wild-type. BI-4732 inhibits EGFR and reduces the phosphorylation of AKT, ERK, and S6K. BI-4732 demonstrates excellent intracranial anti-tumor efficacy in YU-1097 xenograft model harboring EGFR_E19del/T790M/C797S. BI-4732 can be used for the study of non-small cell lung cancer (NSCLC) .
EGFR-IN-23 is a potent EGFR TKI (tyrosine kinase inhibitor) with an IC50 of 8.05 nM for BaF3/EGFR-DEL19/T790M/C797S cell (WO2021244502A1, compound 8) .
EGFR-IN-126 (compound 9d) is a potent inhibitor of EGFR L858R/T790M/C797S, with the IC50 value of 0.005 μM. EGFR-IN-126 shows antitumor effects in vivo and in vitro .
EGFR-IN-22 is a potent EGFR inhibitor with IC50s of 4.91 nM and 0.54 nM for wild type EGFR and EGFR L858R/T790M/C797S, respectively (CN112538072A, compound 243) .
EGFR WT/T790M-IN-3 is an irreversible covalent EGFR WT and EGFR T790M inhibitor with IC50s value of 28.1 and 24.6 nM. EGFR WT/T790M-IN-3 hampers tubulin polymerization through IC50 value of 5.1 μM. EGFR WT/T790M-IN-3 shows significant anti-proliferative effects on HCT116 and T47D cells, with IC50 values of 3.12 and 4.12 μM, respectively. EGFR WT/T790M-IN-3 can be used for the study of cancers such as non-small cell lung cancer, colon cancer and breast cancer .
BLU-945 is a potent, highly selective, reversible and orally active epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKIs). BLU-945 can effectively inhibit EGFR with L858R and/or exon 19 deletion mutation, T790M mutation and C797S mutation. BLU-945 can be used for the research of lung cancer including non-small cell lung cancer (NSCLC) .
EGFR-IN-89 (compound 13k) is a potent, fourth-generation EGFR mutation inhibitor with an IC50 of 10.1 nM against Del19/T790M/C797S mutations. EGFR-IN-89 shows higher selectivity over wild type .
EGFR WT/T790M-IN-1 (Compound 16h) is a dual EGFR WT and EGFR T790 inhibitor. EGFR WT/T790M-IN-1 can arrest the cell cycle in G2/M phase and induce apoptosis. EGFR WT/T790M-IN-1 has anti-cancer activity .
ZSH-2117 is a covalent and selective EGFRPROTAC degrader with a DC50 of 45 nM in Ba/F3-EGFR L858R/T790M/C797S cells. ZSH-2117 significantly inhibits cell proliferation and reduces the downstream EGFR signaling proteins level of AKT and ERK. ZSH-2117 effectively inhibits tumor growth in Ba/F3-EGFR L858R/T790M/C797S xenograft mice model . Pink: EGFR ligand (HY-175162); Blue: NEDD4 ligase ligand (HY-175159); Black: linker
EGFR-IN-120 (Compound 11eg) is an orally active EGFR inhibitor. EGFR-IN-120 inhibits EGFR L858R/T790M/C797S with an IC50 value of 0.053 μM, and has a relatively weak effect on EGFR WT (IC50: 1.05 μM). EGFR-IN-120 inhibits the phosphorylation of EGFR and main downstream effectors (STAT3, AKT, and Erk). EGFR-IN-120 induces cell cycle arrest and cell apoptosis in EGFR mutant cells. EGFR-IN-120 inhibits the proliferation of the NSCLC cells harboring EGFR L858R/T790M/C797S with an IC50 of 0.052 μM .
LSD1/EGFR-IN-1 (compound L-1) is a potent inhibitor of LSD1, EGFR T790M/L858R and EGFR L858R/T790M/C797S, with IC50s of 6.24 and 2.06 and 5.01 μM, respectively. LSD1/EGFR-IN-1 plays an important role in cancer research .
JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFR L858R/T790M. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFR L858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities .
EGFR mutant-IN-1, a 5-methylpyrimidopyridone derivative, is a potent and selective EGFR L858R/T790M/C797S mutant inhibitor with an IC50 of 27.5 nM, while being a significantly less potent for EGFR WT (IC50 >1.0 μM) .
EGFR-IN-30 is a potent EGFR inhibitor with IC50s of 1-10 nM, <1 nM for EGFR (WT), EGFR (L858R/T790M/C797S), respectively. EGFR-IN-30 has potential for cell proliferative diseases, such as cancer research .
EGFR T790M/L858R-IN-3 (compound B1) is a EGFR L858R/T790M inhibitor with IC50 value of 13?nM. EGFR T790M/L858R-IN-3 shows anti-tumour activity in H1975 cells with an IC50 value of 0.087 μΜ. EGFR T790M/L858R-IN-3 inhibits cell migration in A549 cells and induces apoptosis in H1975 cells .
EGFR T790M/L858R-IN-9 (Compound 8) is an EGFR-L858R/T790M inhibitor that demonstrates potent inhibitory phosphorylation effects against the EGFR-L858R/T790M mutant kinase, with an IC50 value of 0.0064µM. EGFR T790M/L858R-IN-9 also inhibits the proliferation of non-small cell lung cancer (NSCLC) cells and can be utilized in cancer research .
EGFR-IN-47 is a potent and orally active EGFR L858R/T790M/C797S inhibitor with an IC50 of 0.01 μM. EGFR-IN-47 induces cell cycle attest and cell apoptosis. EGFR-IN-47 has the potential for the research of NSCLC .
EGFR T790M/L858R-IN-7 (Compound 72) is a novel pyrimidine compound that inhibits the EGFR T790M and L858R mutation with a high efficacy (93% inhibition rate at 0.05 μM). EGFR T790M/L858R-IN-7 functions by specifically binding to the kinase domain of EGFR, thereby inhibiting its phosphorylation activity .
EGFR T790M/L858R-IN-8 (compound 9) is a potent inhibitor of EGFR targeting mutant EGFR T790M/L858R with an IC50 of 56.8 μM. The anti-proliferative effect of EGFR T790M/L858R-IN-8 on cancer cell lines A549, A431, and NHI-H1975 is not significant .
EGFR-IN-127 is an ATP-competitive EGFR inhibitor with IC50s of 136.3 nM and 161. 2 nM for EGFR del19 and EGFR del19/T790M/C797S, respectively. EGFR-IN-127 has the potential for the study of non-small-cell lung cancer (NSCLC) .
EGFR WT/T790M/L858R-IN-1 (compound 10d) is a potent EGFR inhibitor, with IC50s of 0.097, 0.280, and 0.051?μM for EGFR WT, EGFR T790M, and EGFR L858R, respectively. EGFR WT/T790M/L858R-IN-1 can be used for the research of cancer .
EGFR-IN-161 (Compound DD-8) is a potent and reversible inhibitor of L858R/T790M/C797S mutant EGFR kinases, with an IC50 of 0.87 nM. EGFR-IN-161 can induce apoptosis process, G1-phase arrestation, and migration inhibition in tumor cells .
EGFR T790M/L858R-IN-2 is a potent and selective EGFRT790M/L858R inhibitor with IC50 values of 3.5, 1290 nM for EGFRT790M/L858R, EGFR WT, respectively. EGFR T790M/L858R-IN-2 decreases the expression of p-EGFR, P-AKT, P-ERK1/2. EGFR T790M/L858R-IN-2 induces Apoptosis and cell cycle arrest in the G1 phase. EGFR T790M/L858R-IN-2 shows anti-cancer activity .
EGFR-IN-164 (Compound 4) is a selective and covalent allosteric EGFR inhibitor. EGFR-IN-164 significantly inhibits the activity of EGFR L858R/T790M/C797S kinase (IC50: 48.1 nM) and proliferation of of EGFR-mutant cells. EGFR-IN-164 can be used for drug resistance of cancer research .
EGFR-IN-7 is a potent, selective and orally active EGFR kinase inhibitor. EGFR-IN-7 has inhibitory effect for for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) with IC50 values of 7.92 nM and 0.218 nM, respectively. EGFR-IN-7 can be used for the research of various cancers .
BI-4020 is a fourth-generation, orally active, and non-covalent EGFR tyrosine kinase inhibitor. BI-4020 inhibits not only the triple mutant EGFR del19T790M C797S variant (IC50=0.2 nM in BaF3 cell lines) but also the double mutant EGFR del19T790M and primary mutant EGFR del19 (IC50=1 nM). BI-4020 also shows activity against EGFR wt (IC50=190 nM). BI-4020 shows high kinome selectivity and good DMPK properties .
EGFR-IN-160 (Compound R12) is an EGFR inhibitor (IC50 values are 1.62, 0.49 and 0.98 μM for EGFR WT, EGFR T790M and EGFR L858R/T790M/C797S, respectively). EGFR-IN-160 induces G2/M and S phase arrest and apoptosis in NCI-H522 cells, and has anticancer activity. EGFR-IN-160 has antioxidant effects against DPPH (IC50: 12.11 µM) and H2O2 (IC50: 8.89 µM) .
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR d746-750/C797S Recombinant Human Active Protein Kinase is a recombinant EGFR d746-750/C797S protein that can be used to study EGFR d746-750/C797S-related functions .
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR T790M/L858R Recombinant Human Active Protein Kinase is a recombinant EGFR T790M/L858R protein that can be used to study EGFR T790M/L858R-related functions .
EGFR-IN-139 (compound PD 18) is an epidermal growth factor receptor (EGFR) inhibitor, with IC50s of 12.88 (wild type), 10.84 (L858R/T790M), 42.68 (L858R/T790M/C797S) nM, respectively. EGFR-IN-139 displays strong anticancer activity against A549 and H1975 cancer cell lines, which are highly expressed EGFR. EGFR-IN-139 has a strong selectivity to cancer cells. EGFR-IN-139 can be used for nonsmall cell lung cancer (NSCLC) research[1].
EGFR is a driver of tumorigenesis. EGFR is mainly found in an auto-inhibited, dimerization-incompetent, state at the plasma membrane (PM). Ligand binding promotes receptor dimerization, which determines a series of structural rearrangements that are conveyed to the cytoplasmic domain allowing the formation of asymmetric dimers between the two juxtaposed catalytic domains. EGFR has multiple mutants. EGFR C797S/L858R Recombinant Human Active Protein Kinase is a recombinant EGFR C797S/L858R protein that can be used to study EGFR C797S/L858R-related functions .
JBJ-09-063 is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 can be used for researching EGFR-mutant lung cancer .
JBJ-09-063 TFA is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 TFA effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 TFA is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 TFA can be used for researching EGFR-mutant lung cancer .
JBJ-09-063 hydrochloride is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 hydrochloride effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 hydrochloride is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 hydrochloride can be used for researching EGFR-mutant lung cancer .
DA-0157 is the orally active inhibitor for EGFR and ALK that overcomes drug-resistant mutations of EGFR C797S and ALK in NSCLC) cells. DA-0157 inhibits the proliferation of Ba/F3-EGFR Del19/T790M/C797S (IC50 = 6.9 nM), Ba/F3-EGFR WT (IC50 = 0.83 μM), Ba/F3-EML4-ALK-L1196M (IC50 = 5.5 nM), and Ba/F3-EML4-ALK (IC50 = 7.4 nM). DA-0157 inhibits CYP2D6 with IC50 of 5.26 μM. DA-0157 exhibits antitumor efficacy in mouse models .
PROTAC EGFR degrader 14 is a potent and selective EGFR PROTACdegrader with a DC50 of about 2.9 nM and a Dmax of 93.1% for EGFR L858R/T790M/C797S. PROTAC EGFR degrader 14 selectively induces EGFR C797S degradation through a VHL and proteasome-dependent manner and downregulated EGFR-associated transcriptome and exhibits good selectivity over EGFR WT. PROTAC EGFR degrader 14 induces cell cycle arrest and apoptosis and significantly inhibits tumor growth. PROTAC EGFR degrader 14 can be used for the study of nonsmall cell lung cancer (NSCLC) (Pink: Target protein ligand: (HY-143337); Blue: E3 ligand (HY-125845); Black: Linker (HY-W004688)) .
PROTAC EGFR degrader 9 (Compound C6) is an orally active CRBN-based PROTAC EGFR degrader. PROTAC EGFR degrader 9 exhibits a DC50 of 10.2 nM and a Kd of 240.2 nM against EGFR L858R/T790M/C797S. PROTAC EGFR degrader 9 exhibits potent degradation activity against various EGFR mutants, while sparing the EGFRWT. (Blue: CRBN ligand (HY-A0003), Black: linker (HY-161613); Pink: EGFR inhibitor (HY-161537)) .
PROTAC EGFR degrader 13 (compound 106) is an EGFR PROTAC degrader with a DC50 of <0.1 μM. PROTAC EGFR degrader 13 has proliferation inhibitory activity on cell Ba/F3-TEL-EGFR-T790M-L858R-C797S with an IC50 of 15.6 nM. PROTAC EGFR degrader 13 can be used for the study of EGFR-related diseases such as cancer (Pink: Target protein ligand; Blue: E3 ligand (HY-14658); Black: linker (HY-W262798); E3 ligand + linker: HY-W998306) .
Almonertinib (HS-10296) mesylate is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib mesylate shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib mesylate is used for the research of the non-small cell lung cancer .
Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer .
Almonertinib (HS-10296) hydrochloride is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib hydrochloride shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib hydrochloride is used for the research of the non-small cell lung cancer .
EGFR T790M/L858R/ACK1-IN-1 is a dual inhibitor of EGFR T790M/L858R and ACK1. IC50 values are 23 and 263 nM, respectively. EGFR T790M/L858R/ACK1-IN-1 can inhibit cell proliferation and has antitumor activity .
Almonertinib (Standard) is the analytical standard of Almonertinib. This product is intended for research and analytical applications. Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer .
Rociletinib (CO-1686) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.
WZ4002 is a mutant selective EGFR inhibitor with IC50s of 2, 8, 3 and 2 nM for EGFR L858R, EGFR L858R/T790M, EGFR E746_A750 and EGFR E746_A750/T790M, respectively.
BPI-15086 an orally active, potent, irreversible mutant-selective inhibitor of both EGFR and T790M resistance mutations tyrosine kinase. BPI-15086 can be used for the research of non-small-cell lung cancer .
Rociletinib hydrobromide (CO-1686 hydrobromide) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.
WZ3146 is a mutant selective EGFR inhibitor with IC50s of
2, 2, 5, 14 and 66 nM for EGFR L858R, EGFR L858R/T790M, EGFR E746_A750, EGFR E746_A750/T790M and EGFR, respectively.
EGFR-IN-49 is a potent and selective EGFR inhibitor with IC50s of 65.0 nM and 13.6 nM for EGFR T790M and EGFR T790M/L858R, respectively. EGFR-IN-49 induces late apoptosis in a dose-dependent manner .
PF-06459988 is an orally activity, irreversible and mutant-selective inhibitor of EGFR mutant forms. PF-06459988 demonstrates high potency and specificity to the T790M-containing double mutant EGFRs. PF-06459988 can be used for the research of cancer .
AV-412 (MP412) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFR L858R, EGFR T790M, EGFR L858R/T790M and ErbB2, respectively.
Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity .
Rociletinib (Standard) is the analytical standard of Rociletinib. This product is intended for research and analytical applications. Rociletinib (CO-1686) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.
Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
EAI045 is an allosteric and the fourth-generation inhibitor of mutant EGFR with IC50s of 1.9, 0.019, 0.19 and 0.002 μM for EGFR, EGFR L858R, EGFR T790M and EGFR L858R/T790M at 10 μM ATP, respectively.
Osimertinib mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
EGFR-IN-61 (compound 22a) is a potent EGFR kinase inhibitor, with IC50 values of 42 nM (L858R/T790 M), 137 nM (L858R/T790M/C797S), and 743 nM (WT), respectively. EGFR-IN-61 shows antiproliferative activity against A549 and H1975 cell lines, with IC50 values of 2.14 and 1.82 μM, respectively .
YK-029A is an orally active inhibitor of mutant EGFR，targeting to both the T790M mutations (EGFR T790M) and exon 20 insertion of EGFR (EGFRex20ins). YK-029A exhibits significant antitumor activity，and results tumor regression in EGFRex20ins-driven PDX models .
EGFR-IN-56 (Compound 13a) is a potent EGFR inhibitor with IC50 values of 541.7 nM and 132.1 nM against EGFR T790M and EGFR T790M/L858R, respectively. EGFR-IN-56 blocks cancer cells in G2/M phase and induce into late apoptosis .
AV-412 free base (MP-412 free base) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFR L858R, EGFR T790M, EGFR L858R/T790M and ErbB2, respectively.
Mutated EGFR-IN-2 (compound 91) is a mutant-selective EGFR inhibitor extracted from patent WO2017036263A1, which potently inhibits single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M (IC50=＜1nM) and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. Mutated EGFR-IN-2 shows anti-tumor antivity .
limertinib (ASK120067) diTFA is a potent and orally active inhibitor of EGFR T790M (IC50: 0.3 nM) with selectivity over EGFRWT (IC50: 6.0 nM). limertinib diTFA is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC) .
Osimertinib-d6 is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
Rociletinib hydrobromide (Standard) is the analytical standard of Rociletinib hydrobromide. This product is intended for research and analytical applications. Rociletinib hydrobromide (CO-1686 hydrobromide) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.
limertinib (ASK120067) is a potent and orally active inhibitor of EGFR T790M (IC50:0.3 nM) with selectivity over EGFR WT (IC50:6.0 nM). limertinib is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC) .
Osimertinib dimer is a dimer of Osimertinib (HY-15772). Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
Firmonertinib (Alflutinib; Furmonertinib) is an orally active, mutant-selective, and highly brain penetrant EGFR inhibitor. Firmonertinib inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation .
Firmonertinib (Alflutinib; Furmonertinib) mesylate is is an orally active, mutant-selective, and highly brain penetrant EGFR inhibitor. Firmonertinib mesylate inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib mesylate has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation .
EGFR-IN-91 (compound 9) is an orally available EGFR inhibitor with blood-brain barrier penetrability. EGFR-IN-91 inhibits EGFR L858R/C797S and EGFR exon 19del/C797S, inducing tumor regression in xenograft (PDX) mouse models. EGFR-IN-91 has the potential to inhibit localized and metastatic non-small cell lung cancer (NSCLC) driven by EGFR mutants .
Osimertinib (mesylate) (Standard) is the analytical standard of Osimertinib (mesylate). This product is intended for research and analytical applications. Osimertinib mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
Icotinib (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Osimertinib (Standard) is the analytical standard of Osimertinib. This product is intended for research and analytical applications. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
Icotinib Hydrochloride (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib (Hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Mavelertinib is a selective, orally available and irreversible EGFR tyrosine kinase inhibitor (EGFR TKI), with IC50s of 5, 4, 12 and 3 nM for Del, L858R, and double mutants T790M/L858R and T790M/Del, respectively. Mavelertinib can be used for the research of non-small-cell lung cancer (NSCLC) .
EGFR-IN-158 (compound 12e) is an orally active EGFR inhibitor with an IC50 of 0.22 nM for EGFR(Del19/T790M). EGFR-IN-158 inhibits phosphorylation and downstream signaling by binding to EGFR, thereby inhibiting the proliferation of tumor cell lines and promoting apoptosis .
EGFR-IN-1 hydrochloride is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 hydrochloride potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .
PF-6274484 is a potent EGFR inhibitor with Kis of 0.14 nM and 0.18 nM for EGFR-L858R/T790M and WT EGFR, respectively. PF-6274484 inhibits EGFR-L858R/T790M autophosphorylation in H1975 tumor cells and EGFR WT in A549 tumor cells with IC50s of 6.6 and 5.8 nM, respectively .
Icotinib (Standard) is the analytical standard of Icotinib. This product is intended for research and analytical applications. Icotinib (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
EGFR-IN-1 TFA is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .
EGFR-IN-1 (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .
WZ8040 is an irreversible mutated EGFR T790M inhibitor and inhibits EGFR phosphorylation. WZ8040 displays 100-fold greater activity against the mutated EGFR than the normal .
Mutated EGFR-IN-1 (Osimertinib analog) is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant and T790M resistance mutant.
Avitinib (Abivertinib) maleate dihydrate is a third-generation, irreversible and orally active selective EGFR inhibitor, with IC50 values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M and wild-type EGFR. Avitinib maleate dihydrate is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib maleate dihydrate shows anticancer effects .
ALK/EGFR-IN-1 (Compound 8l) is an ALK/EGFR dual inhibitor that blocks the phosphorylation of EGFR and ALK. ALK/EGFR-IN-1 inhibits ALK/EGFR mutants respectively, with IC50 of 4.3 nM for EGFR L858R T790M in H1975 cells and EML4-ALK in BaF3 cells, respectively. and 3.6 nM. ALK/EGFR-IN-1 may be used in NSCLC research .
Icotinib-d4 is the deuterium-labeled Icotinib (HY-15164A). Icotinib-d4 (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib-d4 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Mutant EGFR inhibitor is a potent and selective mutant EGFR inhibitor extracted from patent WO 2013014448 A1; inhibits EGFR L858R, EGFR Exon 19 deletion and EGFR T790M.
EGFR-IN-75 is an EGFR WT and EGFR T790M inhibitor with IC50 values of 0.28 μM and 5.02 μM, respectively. EGFR-IN-75 shows anticancer and antioxidant activity .
EGFR-IN-93 (compound 18) is an allosteric inhibitor of T790M/L858R double mutant EGFR. EGFR-IN-93 can be used for non-small lung cancer (NSCLC) research .
Poziotinib (HM781-36B) is an orally active, irreversible pan-HER inhibitor, which effectively inhibits EGFR wt, HER-2 and HER-4 with IC50s of 3.2, 5.3 and 23.5 nM, respectively. Poziotinib (HM781-36B) also shows excellent inhibitory activities against mutated EGFRs, including EGFR T790M and EGFR L858R/T790M, with IC50s of 4.2 and 2.2 nM, respectively. Excellent antitumor activity .
PROTAC EGFR degrader 12 (example 1) is a PROTAC degrader targeting EGFR that can effectively degrade EGFR mutants, but has little effect on EGFR WT. PROTAC EGFR degrader 12 shows IC50s against EGFR L858R-T790M (NCI-H1975 cells), EGFR L858R (NCI-H3255 cells), and EGFR L858R-T790M-L797S (NCI-H1975+CS cells) of all <50 nM .
Neptinib (NEP010) is an orally active derivative of Afatinib (HY-10261) that has stronger antitumor activity than Afatinib (HY-10261) by improving pharmacokinetics. Neptinib has a significant inhibitory effect on tumor growth in mouse non-small cell lung cancer models with different EGFR mutations. Neptinib has a certain inhibitory effect on the EGFR kinase family, with IC50 values ??of 0.24 nM, 7.25 nM, 0.46 nM and 1.79 nM for EGFRwt, EGFRL858R/T790M, EGFRL858R and EGFRT790M, respectively .
Dacomitinib metabolite M1/2 is a potent inhibitor of both wild-type (WT) EGFR and the T790M mutation, demonstrating significant activity against acquired resistance mechanisms in EGFR-mutant non-small-cell lung cancer (NSCLC).
Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFR L858R and EGFR L858R/T790M, respectively.
EAI001 is a potent, selective mutant epidermal growth factor receptor (EGFR) allosteric inhibitor with an IC50 value of 24 nM for EGFR L858R/T790M. EAI001 can be used for research of cancer .
EGFR-IN-62 (compound 9h) is a potent and reversible EGFR kinase inhibitor, with IC50 values of 10 nM (L858R/T790 M), 29 nM (WT), and 242 nM (L858R/T790M/C797S), respectively. EGFR-IN-62 shows antiproliferative activity against A549 and H1975 cell lines, with IC50 values of 2.53 and 1.56 μM, respectively. EGFR-IN-62 induces dose-dependent apoptosis process, G1/G0-phase arrestation, and the inhibition of motility on A549 and/or H1975 cell lines .
Befotertinib (D-0316) mesylate is an orally active EGFR tyrosine kinase inhibitor. Befotertinib mesylate can inhibit the proliferation of tumor cells. Befotertinib mesylate can be used in the research of EGFR T790M-positive non-small cell lung cancer (NSCLC) .
Befotertinib (D-0316) is an orally active EGFR tyrosine kinase inhibitor. Befotertinib can inhibit the proliferation of tumor cells. Befotertinib can be used in the research of EGFR T790M-positive non-small cell lung cancer (NSCLC) .
T-1-DOCA ia a EGFR inhibitor, with the IC50 of 56.94 and 269.01?nM for EGFR WT and EGFR T790M, respectively. T-1-DOCA can induces cell apoptosis of HCT-116 cells .
CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ～10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) cell lines .
EGFR-IN-60 (Compound 7d) shows obvious inhibition of EGFR WT, EGFR T790M, EGFR L858R and JAK3 with IC50s of 83, 26, 53, and 69 nM, respectively. EGFR-IN-60 potently inhibits the growth of H1975 cells harboring EGFR T790M mutation (IC50=1.32 µM) over A431 cells overexpressing EGFR WT (IC50=4.96 µM). EGFR-IN-60 exhibits good oral absorption, potent and safe antitumor activity. EGFR-IN-60 induces cell death through apoptosis supported by increased Bax/Bcl-2 ratio .
ES-072 is an orally effective selective EGFR mutant (EGFR-T790M) inhibitor. ES-072 activates GSK3α by inhibiting EGFR-T790M activity, which promotes phosphorylation of PD-L1 at Ser279 and Ser283. The phosphorylated PD-L1 recruits the E3 ubiquitin ligase ARIH1, leading to ubiquitination and proteasomal degradation of PD-L1. This mechanism not only reduces cancer cell growth but also enhances anti-tumor immune response by lowering PD-L1 levels. ES-072 can be used to inhibit proliferation in non-small cell lung cancer (NSCLC) cells .
Gozanertinib is an orally active furanopyrimidine-based EGFR inhibitor with IC50s of 15 nM and 48 nM for EGFR WT and EGFR L858R/T790M, respectively. Gozanertinib can occupy the ATP-binding site. Gozanertinib has significant antitumor efficacy .
AST5902 mesylate is a principal metabolite of Alflutinib, exhibiting significant antineoplastic activity. AST5902 mesylate contributes to the overall pharmacological effects in the treatment of non-small cell lung cancer. AST5902 mesylate is involved in the response to activating EGFR mutations and can help overcome EGFR T790M drug-resistant mutations.
EGFR-IN-9 (Compound 8) is a potent EGFR kinase inhibitor with IC50s of 7 nM, 28 nM for the wild type EGFR kinase and double mutant EGFR kinase (L858R/T790M). EGFR-IN-9 has antitumor activity .
EGFR-IN-78 (compound A5)，a 2-aminopyrimidine derivative，is a reversible inhibitor of EGFRC797S-TK，and also an inducer of apoptosis. EGFR-IN-78 shows anti-proliferative activity，inhibits EGFR phosphorylation and arrests cell cycle at G2/M phase .
Afatinib-d4 is the deuterium labeled Afatinib. Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.
Afatinib impurity 11 is an impurity of Afatinib. Afatinib is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively .
JNK3 inhibitor-2 is a potent and selective JNK3 inhibitor with IC50 values of >100, >100, 0.25 µM for JNK1, JNK2, JNK3, respectively. JNK3 inhibitor-2 shows DDR1 and EGFR (T790M, L858R) inhibition .
DY3002 is a selective and highly potent EGFR inhibitor with activity in overcoming T790M-mediated drug resistance in non-small cell lung cancer. DY3002 exhibited superior inhibitory effects against EGFR T790M mutants in kinase assays (IC50 = 0.71 nM), compared to weaker inhibitory effects against wild-type EGFR (IC50 = 448.7 nM). DY3002 was significantly superior to rociletinib and osimertinib in selectivity, showing an extremely high selectivity index (SI = 632.0). In cell experiments, DY3002 had an IC50 value of 0.037 μM against H1975 cells, showing enhanced inhibitory potency. In addition, DY3002 was superior to other alternative compounds in terms of biological properties and did not cause hyperglycemia .
EGFR ligand-2 (compound C4), a covalent EGFR ligand, is a EGFR mutant inhibitor with IC50s of 21 nM and 48 nM for EGFR L858R and EGFR L858R/T790M, respectively. EGFR ligand-2 can be used to synthesize PROTAC .
Osimertinib (dimesylate) (Standard) is the analytical standard of Osimertinib (dimesylate). This product is intended for research and analytical applications. Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively.
EGFR/VEGFR2-IN-5 (Compound 14) is an orally active dual inhibitor of EGFR and VEGFR2 with an IC50 value of 1.15 µM for VEGFR2 and an IC50 value of 0.28 μM for EGFR T790M. EGFR/VEGFR2-IN-5 has significant anticancer activity .
Afatinib-d6 (dimaleate) is the deuterium labeled Afatinib dimaleate. Afatinib dimaleate is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively .
Osimertinib- 13C,d3 is the deuterium and 13C labeled Osimertinib. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively.
AZ-5104 is an active, demethylated metabolite of AZD 9291. AZ-5104 is an EGFR inhibitor with IC50s of 1, 6, 1, 25 and 7 nM for EGFR L858R/T790M, EGFR L858R, EGFR L861Q, EGFR and ErbB4, respectively.
EGFR-IN-52 (Compound 4) is a potent EGFR inhibitor with IC50 values of 0.358, 86.02 and 432.67 µM against EGFR, EGFR L858R-TK and EGFR T790M-TK, respectively. EGFR-IN-52 shows cytotoxic activity against cancer cell lines and induces apoptosis .
AZ-5104-d2 is the deuterium labeled AZ-5104. AZ-5104 is an EGFR inhibitor with IC50s of 1 nM, 6 nM, 1 nM, 25 nM and 7 nM for EGFRL858R/T790M, EGFRL858R, EGFRL861Q, EGFR and ErbB4, respectively .
EGFR-IN-96 (compound 7a) is a thieno[2,3-d]pyrimidine EGFR inhibitor that can induce apoptosis. EGFR-IN-96 arrests the growth of HepG2 cells in the S phase and G2/M phase, and inhibits the growth of cancer cells bearing EGFR wild-type and EGFR T790M .
EGFR-IN-109 (compound 4) is an EGFR inhibitor, with the IC50 values of 25.8 and 182.3 nM for EGFR WT and EGFR T790M, respectively. EGFR-IN-109 arrests the cancer cells’ growth at the G2/M phase and induces both early and late apoptosis. EGFR-IN-109 can be used in cancer research .
EGFR-IN-51 (Compound 6) is a potent EGFR inhibitor with IC50 values of 0.493, 102.60 and 461.63 µM against EGFR, EGFR L858R-TK and EGFR T790M-TK, respectively. EGFR-IN-51 shows cytotoxic activity against cancer cell lines and induces apoptosis .
DS06652923 is an orally active EGFR triple mutation inhibitor. DS06652923 has a growth inhibition effect on Ba/F3 EGFR del19/T90M/C797S cells, with a GI50 value of 9.4 nM. DS06652923 can lead to tumor regression in Ba/F3 xenograft models .
Avitinib (Abivertinib) maleate is a third-generation, irreversible and orally active selective EGFR inhibitor, with IC50 values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M and wild-type EGFR. Avitinib maleate is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib maleate shows anticancer effects .
EGFR-IN-55 (Compound 8a) is a potent EGFR inhibitor with IC50 values of 70 nM and 3.9 nM against EGFR WT and EGFR L858R/T790M, respectively. EGFR-IN-55 arrests NCI-H1975 cells in G0/G1 phase and shows anticancer activity .
Avitinib (Abivertinib) is a third-generation, irreversible and orally active selective EGFR inhibitor, with IC50 values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M and wild-type EGFR. Avitinib is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib shows anticancer effects .
pan-HER-IN-1 (Compound C5) is an irreversible, orally active pan-HER inhibitor with IC50 values of 0.38, 1.6, 2.2 and 3.5 nM against EGFR, HER4, EGFR T790M/L858R and HER2, respectively. pan-HER-IN-1 induces apoptosis and shows antitumor activities .
pan-HER-IN-2 (Compound C6) is a reversible, orally active pan-HER inhibitor with IC50 values of 0.72, 2.0, 8.2 and 75.1 nM against EGFR, HER4, EGFR T790M/L858R and HER2, respectively. pan-HER-IN-2 induces apoptosis and shows antitumor activities .
(3S, 4S)-PF-06459988 is the S enantiomer of PF-06459988 with less active. PF-06459988 is a potent irreversible inhibitor of T790M mutant epidermal growth factor receptor (EGFR). PF-06459988 has excellent selectivity against EGFR wild-type while possessing a minimally reactive electrophile that reduces the propensity of off-target labeling .
EGFR-IN-81 (Compound 10i) is an EGFR inhibitor. EGFR-IN-81 inhibits EGFR WT and L858R/T790M with IC50s 4.38 nM and 5.69 nM. EGFR-IN-81 has cytotoxic activity against MCF-7 and HCT116 cells with of 2.07 μM and 6.72 μM respectively .
(S)-Sunvozertinib ((S)-DZD9008), the S-enantiomer of Sunvozertinib, shows inhibitory activity against EGFR exon 20 NPH and ASV insertions, EGFR L858R/T790M mutation and Her2 exon20 YVMA insertion (IC50=51.2 nM, 51.9 nM, 1 nM, and 21.2 nM, respectively). (S)-Sunvozertinib also inhibits BTK .
EGFR-IN-107 (compound 3r) is an orally active EGFR inhibitor with IC50 values of 0.4333 μM for EGFR WT and 0.0438 μM for EGFR L858R/T790M. EGFR-IN-107 has anti-proliferative activity and can inhibit the proliferation of H1975 cells and induce their apoptosis. EGFR-IN-107 can be used in cancer research .
EGFR/HER2-IN-5 (compound 6h) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-5 inhibits EGFR with an IC50 value of 1.01 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-5 has potent antitumor efficacy in vivo and can be used for lung cancer research .
EGFR/HER2-IN-4(compound 6d) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-4 inhibits EGFR with an IC50 value of 0.6 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-4 has potent antitumor efficacy in vivo and can be used for lung cancer research .
EGFR-TK-IN-1 (compound 7o) is a potent mutant EGFR inhibitor with IC50 of 8.5 nM an 9.3 nM against EGFR L858R/T790M and EGFR Del19.EGFR-TK-IN-1 showes strong antiproliferative effects against EGFR mutant-driven non-small cell lung cancer (NSCLC) cells and induces cell apoptosis .
JBJ-07-149 is an inhibitor for EGFRL858R/T790M with an IC50 of 1.1 nM. JBJ-07-149 inhibits the proliferation of cell Ba/F3 with IC50 of 4.9 μM and 0.148 μM, without and with presence of Cetuximab (HY-P9905). JBJ-07-149 can be used as ligand for target protein in synthesis of DDC-01-163 (HY-139997) .
Theliatinib (Xiliertinib) tartrate is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases . Theliatinib (tartrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Icotinib (Hydrochloride) (Standard) is the analytical standard of Icotinib (Hydrochloride). This product is intended for research and analytical applications. Icotinib Hydrochloride (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFRL858R, EGFRL858R/T790M, EGFRT790M and EGFRL861Q. Icotinib (Hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Sunvozertinib (DZD9008) is a potent ErbBs (EGFR, Her2, especially mutant forms) and BTK inhibitor. Sunvozertinib shows IC50s of 20.4, 20.4, 1.1, 7.5, and 80.4 nM for EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, and Her2 Exon20 YVMA, and EGFR WT A431, respectively (patent WO2019149164A1, example 52) .
PROTAC EGFR degrader 4 is a potent PROTAC targeting mutant EGFR.PROTAC EGFR degrader 4 induces EGFR del19 and EGFR L858R/T790M degradation with DC50s of 0.51 and 126 nM, respectively. PROTAC EGFR degrader 4 significantly inhibits growth of HCC827 and H1975 cell lines with IC50s of 0.83 and 203.1 nM, respectively. Induced EGFR degradation is related to autophagy .
Theliatinib (Xiliertinib) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases . Theliatinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
EGFR/PI3Kα-IN-1 (compound 30k) is a dual EGFR/PI3Kα inhibitor with IC50 values of 3.6 nM (EGFRL858R/T790M) and 30 nM (PI3Kα), respectively. EGFR/PI3Kα-IN-1 can inhibit tumor cell proliferation and has anticancer activity .
Afatinib (BIBW 2992) dimaleate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
Afatinib (BIBW 2992) oxalate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib oxalate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
EGFR/BRAFV600E-IN-2 (compound 3g) is a potential multi-target inhibitor of EGFR, BRAF V600E, and EGFR T790M, and an inducer of apoptosis. EGFR/BRAFV600E-IN-2 can activate caspase-3, 8, and Bax, and downregulate the anti-apoptotic protein Bcl2, inducing apoptosis. EGFR/BRAF V600E-IN-2 also has antioxidant activity and DPPH free radical scavenging potency .
Afatinib (Standard) is the analytical standard of Afatinib. This product is intended for research and analytical applications. Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
Afatinib (Standard) is the analytical standard of Afatinib. This product is intended for research and analytical applications. Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
MG-3C is a potent matrix metalloproteinase 9 (MMP-9) inhibitor. MG-3C can selectively kill non-small-cell lung cancer (NSCLC) cells harboring the EGFR T790M mutation. MG-3C blocks the EGFR/STAT3 signaling pathway, inducing G2/M phase arrest, growth inhibition, and apoptosis of cancer cells. MG-3C is promising for research of lung cancer .
Tyrosine kinase-IN-7 (compound 13h) is an inhibitor of the tyrosine kinase EGFR. The IC50s for inhibiting EGFR(WT) and EGFR(T790M) are 0.630 μM and 0.956 μM respectively. Tyrosine kinase-IN-7 has antitumor activity against four cancer cell lines (HepG2, HCT-116, MCF-7, and A431) with IC50s of 13.02 μM, 10.14 μM, 12.68 μM, and 47.05 μM, respectively .
EGFR-IN-1671 is a selective EGFR inhibitor with an IC50 of 0.19 nM. EGFR-IN-167 exhibits good potency against various EGFR mutants (IC50 = 0.109 nM, 0.75 nM and <0.05 nM against EGFR (L858R), EGFR (C797S) and EGFR (del19), respectively). EGFR-IN-1671 covalently engages the catalytically conserved lysine of EGFR in live mammalian cells. EGFR-IN-1671 demonstrates excellent anti-proliferative activity by inhibiting EGFR autophosphorylation. EGFR-IN-1671 can be used for the study of non-small-cell lung carcinomas (NSCLC), glioblastoma and many solid tumors .
Afatinib (dimaleate) (Standard) is the analytical standard of Afatinib (dimaleate). This product is intended for research and analytical applications. Afatinib (BIBW 2992) dimaleate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
(R)-Afatinib ((R)-BIBW 2992) is the Afatinib isomer. Afatinib (HY-10261) is an orally active, potent and irreversible dual specificity inhibitor of?ErbB?family (EGFR?and?HER2), with?IC50?values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for?EGFR wt, EGFR L858R,?EGFR L858R/T790M?and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung?cancer?(NSCLC) and gastric?cancer .
EGFR-IN-165 is a potent EGFR inhibitor. EGFR-IN-165 demonstrates superior potency with IC50s of 17.18 and 64.74 nM against EGFR L858R/T790M and EGFR WT; 2.17 and 6.2 μM against NCI-H1975 cells and A431 cells. EGFR-IN-165 significantly inhibits the migration and induces G1 phase cell cycle arrest and cell apoptosis. EGFR-IN-165 can be used for the study of cancers such as non-small cell lung cancer, colorectal cancer, and head and neck squamous cell carcinoma .
PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFRL858R/T790M degrader, with a DC50 of 13 .2 nM.PROTAC EGFR degrader 7 inhibits NCI-H1975 cells proliferation, with an IC50 of 46 .82 nM.PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI-H1975 cell.PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research .
MAPK-IN-2 (compound 3h) is a potent MAPK inhibitor with antineoplastic activity. MAPK-IN-2 inhibits cancer cell proliferation among serval cancer cell lines, and suppresses MAPK pathway with potant efficacy (EGFR WTIC50=281 nM, c-MET IC50=205 nM, B-RAF WTIC50=112 nM, and CDK4/6 IC50=95 and 184 nM, respectively). MAPK-IN-2 even shows a remarkable potency against mutated EGFR and B-RAF (EGFR T790MIC50=69 nM and B-RAF V600EIC50=83 nM) .
Antiproliferative agent-34 (Compound A14) is a multi-target kinase inhibitor, with an IC50 of 177 nM and 1567 nM for EGFR L858R/T790M and EGFR WT. Antiproliferative agent-34 also inhibits JAK2, ROS1, FLT3, FLT4, PDGFRα with IC50 of 30.93, 106.90, 108.00, 226.60, 42.53 nM. Antiproliferative agent-34 inhibits H1975 and HCC827 cells proliferation with IC50 values below 40 nM under normoxic condition, and the anti-proliferation potency achieves 4–6-fold improvement (IC50 values < 10 nM) under hypoxic condition .
PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFR L858R/T790M degrader, with a DC50 of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cells proliferation, with an IC50 of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research . PROTAC EGFR degrader 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
EGFR/COX-2-IN-1 is an EGFR/COX-2 inhibitor. EGFR/COX-2-IN-1 inhibits EGFR WT, EGFR T790M, COX-1 and COX-2 with IC50s of 0.12, 0.076, 20.1 and 1.52 μM respectively. EGFR/COX-2-IN-1 inhibits and with IC50s of , respectively. EGFR/COX-2-IN-1 inhibits MCF-7, HT-29 and A-549 with IC50s of 1.20, 5.14 and 14.81 μM, respectively. EGFR/COX-2-IN-1 displays Apoptosis induction by up-regulating Bax and down-regulating Bcl-2 protein levels. EGFR/COX-2-IN-1 results in a significant increase in the percentage of cells at the G2/M in MFC-7 cells. EGFR/COX-2-IN-1 exhibits broad-spectrum antitumor effects .
Oritinib (SH-1028) mesylate is a selective, orally active, and pyrimidine-based irreversible inhibitor of EGFR with an IC50 of 18 nM. Oritinib (SH-1028) mesylate exhibits potent activity against EGFR sensitive and resistant (T790 M) mutations. Oritinib (SH-1028) mesylate significantly inhibits proliferation of tumor cells with EGFR sensitive and resistant mutation .
Afatinib (Standard) is the analytical standard of Afatinib. This product is intended for research and analytical applications. Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
The EGFR protein is a receptor tyrosine kinase that can bind to a variety of ligands, such as EGF, TGFA, AREG, epigen, BTC, epiregulin, and HBEGF, to initiate signaling cascades that mediate cellular responses. This involves receptor dimerization, autophosphorylation and recruitment of adapter proteins such as GRB2, activating downstream pathways such as RAS-RAF-MEK-ERK, PI3-kinase-AKT, PLCgamma-PKC and STAT. EGFR Protein, Human (T790M, L858R, sf9, Strep, GST, His) is the recombinant human-derived EGFR, expressed by Sf9 insect cells , with C-8*His, N-GST, N-Strep labeled tag. ,
The EGFR protein is a receptor tyrosine kinase that can bind to a variety of ligands, such as EGF, TGFA, AREG, epigen, BTC, epiregulin, and HBEGF, to initiate signaling cascades that mediate cellular responses. This involves receptor dimerization, autophosphorylation and recruitment of adapter proteins such as GRB2, activating downstream pathways such as RAS-RAF-MEK-ERK, PI3-kinase-AKT, PLCgamma-PKC and STAT. EGFR Protein, Human (C797S, T790M, L858R, sf9, GST) is the recombinant human-derived EGFR, expressed by Sf9 insect cells, with N-GST labeled tag.
Osimertinib-d6 is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
Osimertinib- 13C,d3 is the deuterium and 13C labeled Osimertinib. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively.
Icotinib-d4 is the deuterium-labeled Icotinib (HY-15164A). Icotinib-d4 (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib-d4 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Afatinib-d4 is the deuterium labeled Afatinib. Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.
Afatinib-d6 (dimaleate) is the deuterium labeled Afatinib dimaleate. Afatinib dimaleate is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively .
AZ-5104-d2 is the deuterium labeled AZ-5104. AZ-5104 is an EGFR inhibitor with IC50s of 1 nM, 6 nM, 1 nM, 25 nM and 7 nM for EGFRL858R/T790M, EGFRL858R, EGFRL861Q, EGFR and ErbB4, respectively .
Icotinib (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Icotinib Hydrochloride (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib (Hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Theliatinib (Xiliertinib) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases . Theliatinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFR L858R/T790M degrader, with a DC50 of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cells proliferation, with an IC50 of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research . PROTAC EGFR degrader 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Theliatinib (Xiliertinib) tartrate is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases . Theliatinib (tartrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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