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Mutant EGFR inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	EGFR (116) Akt (5) Anaplastic lymphoma kinase (ALK) (4) Apoptosis (17) Autophagy (1) BCRP (1) BMX Kinase (1) Btk (2) c-Kit (1) Cannabinoid Receptor (1) Caspase (1) Cytochrome P450 (1) Drug Derivative (1) Endogenous Metabolite (1) ERK (5) Estrogen Receptor/ERR (1) FAK (2) Ferroptosis (1) Glutathione Peroxidase (1) GSK-3 (1) Isotope-Labeled Compounds (1) JAK (2) MEK (1) mTOR (2) p38 MAPK (1) PD-1/PD-L1 (1) Phosphatase (1) PROTACs (8) Reactive Oxygen Species (ROS) (1) Reference Standards (3) ROS Kinase (1) SHP2 (1) SOS1 (1) STAT (2) TAM Receptor (1) Trk Receptor (1) VEGFR (1)
By Research Areas:	Cancer (122) Inflammation/Immunology (2)
Click Chemistry:	Alkynes (4)

124

Inhibitors & Agonists

Inhibitory Antibodies

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: EGFR

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13984

**Mutant EGFR inhibitor** 1 Publications Verification	EGFR	Cancer
Mutant EGFR inhibitor (Example 25) is a potent mutant *EGFR* inhibitor. Mutant EGFR inhibitor inhibits FGFR ^WT with an IC₅₀ of 0.41 nM. Mutant EGFR inhibitor inhibits EGFR ^L858R, EGFR ^{Exon 19 deletion} and EGFR ^T790M. Mutant EGFR inhibitor can be used for the study of diseases mediated by EGFR (particularly cancers) .

HY-155005

EGFR mutant-IN-2	EGFR	Cancer
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 .

HY-19803

Naquotinib mesylate 5 Publications Verification ASP8273 mesylate	EGFR	Cancer
Naquotinib mesylate (ASP8273 mesylate) is an orally available, mutant-selective and irreversible *EGFR* inhibitor; with IC₅₀s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.

HY-19729

Naquotinib 5 Publications Verification ASP8273	EGFR	Cancer
Naquotinib (ASP8273) is an orally available, mutant-selective and irreversible *EGFR* inhibitor; with IC₅₀s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.

HY-131066

EMI48	EGFR	Cancer
EMI48, the derivative of EMI1, displays greater potency toward mutant *EGFR* than EMI1. EMI48 inhibits *EGFR* triple mutants .

HY-131067

EMI56	EGFR	Cancer
EMI56, the derivative of EMI1, displays greater potency toward mutant *EGFR* than EMI1. EMI56 inhibits *EGFR* triple mutants .

HY-78869

Mutated EGFR-IN-1 1 Publications Verification Osimertinib analog	EGFR	Cancer
Mutated EGFR-IN-1 (Osimertinib analog) (Intermediate 168) is an intermediate of the mutant *EGFR* inhibitor.

HY-100520

EGFR-IN-2	EGFR	Cancer
EGFR-IN-2 is a a noncovalent, irreversible, mutant-selective second generation *EGFR* inhibitor.

HY-128860

Mutated EGFR-IN-2	EGFR	Cancer
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 .

HY-162300

EGFR kinase inhibitor 4	EGFR	Cancer
EGFR kinase inhibitor 4 (Compound 4) is a bivalent ATP-allosteric *EGFR* inhibitor (IC₅₀: 1.8 nM for mutant EGFR (LRTMCS)). EGFR kinase inhibitor 4 can be used for research of NSCLC .

HY-12872

Nazartinib 5+ Cited Publications EGF816	EGFR	Cancer
Nazartinib (EGF816) is a covalent mutant-selective *EGFR* inhibitor, with K_i and K_inact of 31 nM and 0.222 min ⁻¹ on EGFR(L858R/790M) mutant, respectively.

HY-13897

CNX-2006	EGFR	Cancer
CNX-2006 is a mutant-selective and irreversible *EGFR* inhibitor with an IC₅₀ below 20 nM for EGFR ^T790M.

HY-161030

EGFR-IN-92	EGFR	Cancer
EGFR-IN-92 (compound 15) is an allosteric T790M/L858R double mutant EGFR inhibitor. EGFR-IN-92 shows antiproliferative activity against H1975 non-small lung cancer (NSCLC) cancer cells expressing double mutant EGFR .

HY-12872A

Nazartinib mesylate EGF816 mesylate	EGFR	Cancer
Nazartinib mesylate (EGF816 mesylate) is a novel, covalent mutant-selective *EGFR* inhibitor, with K_i and K_inact of 31 nM and 0.222 min ⁻¹ on EGFR(L858R/790M) mutant, respectively.

HY-19985

PF-06459988	EGFR	Cancer
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 .

HY-101522

CHMFL-EGFR-202	EGFR BMX Kinase Btk MEK	Cancer
CHMFL-EGFR-202 is a potent, irreversible inhibitor of *epidermal growth factor receptor (EGFR) mutant* kinase, with IC₅₀*s 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 .

HY-19617A

EGFR-IN-1 hydrochloride	EGFR	Cancer
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 .

HY-157526

EGFR-TK-IN-1	EGFR Apoptosis	Cancer
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 .

HY-19617B

EGFR-IN-1 TFA	EGFR	Cancer
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 .

HY-19617

EGFR-IN-1	EGFR	Cancer
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 .

HY-134877

BAY 2476568	EGFR ERK Akt	Cancer
BAY 2476568 is a potent and mutant-selective inhibitor targeting EGFR exon20 insertion variants. BAY 2476568 potently inhibits the kinase activity of EGFR exon20 insertion mutants (insASV, insSVD, insNPG) with IC₅₀ values of 0.09 nM, 0.21 nM, and 0.11 nM, respectively. BAY 2476568 inhibits *EGFR* (Y1068) phosphorylation and reduces the phosphorylation of ERK1/2 and Akt (S473) in Ba/F3 cells expressing EGFR exon20 insertion mutants (insASV, insSVD). BAY 2476568 can be used for the study of non-small cell lung cancer (NSCLC) driven by EGFR exon20 insertion mutations .

HY-W423595

BEBT-109	EGFR	Cancer
BEBT-109 is a potent pan-mutant-selective *EGFR* inhibitor. BEBT-109 has improved pharmacokinetic properties. BEBT-109 can be used for multiple mutant-EGFR-driven non-small cell lung cancer (NSCLC) research .

HY-125841

EGFR mutant-IN-1	EGFR	Cancer
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) .

HY-129550

BI-4020	EGFR	Cancer
BI-4020 is a fourth-generation, orally active, and non-covalent *EGFR* tyrosine kinase inhibitor. BI-4020 inhibits not only the triple mutant EGFR del19 T790M C797S variant (IC₅₀=0.2 nM in BaF3 cell lines) but also the double mutant EGFR del19 T790M 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 .

HY-150905

EGFR ligand-2	EGFR	Cancer
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 .

HY-17654

BIEGi-1	EGFR mTOR	Cancer
BIEGi-1 is an *EGFR* inhibitor. BIEGi-1 effectively disrupts the *EGFR-Rheb* interaction in cells. BIEGi-1 robustly inhibits *EGFR* kinase activity (reduces p-Y1068-EGFR) as well as mTORC1 activation (reduces p-T389-S6K1) in EGFR-mutant cells. BIEGi-1 shows strong antiproliferative effects on EGFR-mutant PC9 and HCC827 cells with IC₅₀ values of 17 nM and 20 nM, respectively. BIEGi-1 can be used for the study of cancers harboring EGFR mutations, such as non-small cell lung cancer (NSCLC) .

HY-18213

EGFR-IN-9	EGFR	Cancer
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 .

HY-161031

EGFR-IN-93	EGFR	Cancer
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 .

HY-161602

EGFR/HER2-IN-13	EGFR	Cancer
EGFR/HER2-IN-13 (Compd 38) is an inhibitor of **mutant EGFR/HER2s** which are resistant to other drugs. EGFR/HER2-IN-13 can be used for cancer research .

HY-161603

EGFR/HER2-IN-14	EGFR	Cancer
EGFR/HER2-IN-14 (Compd 46) is an inhibitor of **mutant EGFR/HER2s** which are resistant to other drugs. EGFR/HER2-IN-14 can be used for cancer research .

HY-178057

EGFR-IN-176	EGFR Akt Anaplastic lymphoma kinase (ALK) Apoptosis	Cancer
EGFR-IN-176 is an orally active and ATP-competitive *EGFR* mutant inhibitor (particularly C797S-mediated EGFR triple mutant). EGFR-IN-176 effectively inhibits subsequent AKT signaling and induces apoptosis in Ba/F3 and PC-9 cells expressing EGFR ^{19del/T790M/C797S} and EGFR ^{L858R/T790M/C797S}. EGFR-IN-176 selectively inhibits EGFR signaling in cell lines harboring EGFR triple mutation and shows no inhibitory effect against A431 cells that express wild-type EGFR. EGFR-IN-176 can effectively inhibit the enzymatic activity of ALK (IC₅₀ < 0.5 nM). EGFR-IN-176 can be used for the study of non-small cell lung cancer (NSCLC) .

HY-174826

EGFR-IN-164	EGFR c-Kit	Cancer
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 .

HY-P99849

Depatuxizumab ABT-806	EGFR	Cancer
Depatuxizumab is a brain-penetrant and humanized tumor-specific anti *EGFR* monoclonal antibody. Depatuxizumab inhibits the growth of xenograft models of mutant EGFRvIII and wild-type EGFR. Depatuxizumab can be used for research on cancer .

HY-139884

EGFR-IN-18	EGFR	Cancer
EGFR-IN-18 potently inhibits enzymatic activity in L858R/T790M/C797S mutant *EGFR* (4.9 nM), with a significantly lower activity for wild-type *EGFR* (47 nM).

HY-79077

Osimertinib dimesylate Maximum Cited Publications 156 Publications Verification AZD-9291 dimesylate; Mereletinib dimesylate	EGFR	Cancer
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.

HY-155227

ALK/EGFR-IN-1	Anaplastic lymphoma kinase (ALK) EGFR Apoptosis	Cancer
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 .

HY-149695

EGFR-IN-91	EGFR	Cancer
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 .

HY-135914

JBJ-02-112-05	EGFR	Cancer
JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active *EGFR* inhibitor with an IC₅₀ of 15 nM for EGFR ^L858R/T790M .

HY-175864

EGFR-IN-173	EGFR Apoptosis p38 MAPK ERK Akt STAT	Cancer
EGFR-IN-173 is an orally active, pan-mutant *EGFR* tyrosine kinase inhibitor that targets EGFR 19del, L858R/T790M and C797S triple-mutations, potently inhibiting EGFR ^{19del/T790M/C797S} with an IC₅₀ of 1.19 nM while showing over 100-fold selectivity for mutant over wild-type EGFR (IC₅₀ = 19.362 μM against WT). EGFR-IN-173 significantly inhibits cell migration, induces apoptosis in non-small cell lung cancer (NSCLC) cells. EGFR-IN-173 inhibits EGFR phosphorylation and suppresses the downstream pathways (MAPK/ERK, AKT, STAT3). EGFR-IN-173 exhibits antitumor efficacy in NSCLC and Ba/F3 xenograft models. EGFR-IN-173 can be used for NSCLC research .

HY-100213

EAI045 3 Publications Verification	EGFR	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.

HY-161633

PROTAC EGFR degrader 11	PROTACs EGFR FAK	Cancer
PROTAC EGFR degrader 11 (Compound B71) is a PROTAC degrader for epidermal growth factor receptor (EGFR), with DC₅₀ <100 nM. PROTAC EGFR degrader 11 binds CRBN-DDB1 with a K_i of 36 nM. PROTAC EGFR degrader 11 degrades EGFR, focal adhesion kinase (FAK), and RSK1, inhibits the proliferation of BaF3 wild type and EGFR mutants, with IC₅₀ <100 nM.

HY-123766

EGFR-IN-99	EGFR	Cancer
EGFR-IN-99 (compound 1a) is a potent *EGFR* and HER2 Exon 20 insertion mutant inhibitor. EGFR-IN-99 has excellent antiproliferative activity against DFCI127 cells, with an EC₅₀ of 11.5 nM. EGFR-IN-99 can be used for the research of non-small cell lung cancer (NSCLC) .

HY-157229

STX-721 1 Publications Verification	EGFR ERK	Cancer
STX-721 is an orally active, irreversible, covalent *EGFR* exon 20 insertion (ex20ins) inhibitor that selectively targets ex20ins-mutant dynamic protein states. STX-721 potently inhibits the kinase activity of EGFR ex20ins mutants (NPG, ASV, SVD). STX-721 inhibits phosphorylation of *EGFR* (pEGFR Y1068) and downstream ERK (pERK Thr202/Tyr204), and suppresses proliferation of ex20ins-mutant Ba/F3 cells and human NSCLC cell lines (NCI-H2073 ASV KI, CUTO-14 ASV). STX-721 induces tumor regression in EGFR ex20ins-mutant PDX/CDX models. STX-721 can be used for the study of non-small cell lung cancer (NSCLC) harboring EGFR or HER2 ex20ins mutations .

HY-12001

WZ-3146	EGFR	Cancer
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.

HY-128862

EGFR-IN-7	EGFR	Cancer
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 .

HY-161632

PROTAC EGFR degrader 10	PROTACs EGFR FAK	Cancer
PROTAC EGFR degrader 10 (Compound B56) is a PROTAC degrader for epidermal growth factor receptor (EGFR), with DC₅₀ <100 nM. PROTAC EGFR degrader 10 binds CRBN-DDB1 with a K_i of 37 nM. PROTAC EGFR degrader 10 degrades EGFR, focal adhesion kinase (FAK), and RSK1, inhibits the proliferation of BaF3 wild type and EGFR mutants, with IC₅₀ <150 nM .

HY-130616

EGFR-IN-11	EGFR Apoptosis	Cancer
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 .

HY-170497

EGFR-IN-140	EGFR	Cancer
EGFR-IN-140 (Compound 31) is the inhibitor for *EGFR, that inhibits* EGFR wildtype and EGFR L858R/T790M/C797S mutant with K_i 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 .

HY-17499

EGFR-IN-12	EGFR Apoptosis	Cancer
EGFR-IN-12 is a 4,6-disubstituted pyrimidine and is a potent, ATP-competitive, irreversible and highly selective *EGFR* inhibitor with an IC₅₀of 21 nM. EGFR-IN-12 also inhibits mutant EGFR ^L858R and EGFR ^L861Q with IC₅₀s of 63 nM and 4 nM, respectively. EGFR-IN-12 displays strong selectivity for *EGFR* over HER4 (IC₅₀ = 7640 nM) and a panel of 55 other kinases. EGFR-IN-12 induces cells apoptosis and has antitumor activity .

HY-168112

EGFR-IN-127	EGFR	Cancer
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) .

Cat. No.	Product Name	Target	Research Area

HY-P99849

Depatuxizumab ABT-806	EGFR	Cancer
Depatuxizumab is a brain-penetrant and humanized tumor-specific anti *EGFR* monoclonal antibody. Depatuxizumab inhibits the growth of xenograft models of mutant EGFRvIII and wild-type EGFR. Depatuxizumab can be used for research on cancer .

Cat. No.	Product Name	Chemical Structure

HY-15772S

Osimertinib-d6
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 .

HY-15772S1

Osimertinib-13C,d3
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.

HY-15164AS

Icotinib-d4

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.

Cat. No.	Product Name		Classification

HY-15164A

Icotinib 5+ Cited Publications BPI-2009		Alkynes
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.

HY-15164

Icotinib Hydrochloride 5+ Cited Publications BPI-2009H		Alkynes
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.

HY-104066

Theliatinib Xiliertinib; HMPL-309		Alkynes
Theliatinib (Xiliertinib) is a potent, ATP-competitive, orally active and highly selective *EGFR* inhibitor with a K_i 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.

HY-104066A

Theliatinib tartrate Xiliertinib tartrate; HMPL-309 tartrate		Alkynes
Theliatinib (Xiliertinib) tartrate is a potent, ATP-competitive, orally active and highly selective *EGFR* inhibitor with a K_i 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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