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Pathways Recommended:	Stem Cell/Wnt Cell Cycle/DNA Damage

Results for "

H1975 cells

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Ack1 (1) Akt (6) Anaplastic lymphoma kinase (ALK) (6) AP-1 (1) Apoptosis (25) Autophagy (3) Caspase (1) CDK (1) Deubiquitinase (2) DNA/RNA Synthesis (2) Drug Metabolite (1) E1/E2/E3 Enzyme (1) EGFR (43) Endogenous Metabolite (1) ERK (2) Ferroptosis (2) HDAC (2) HIF/HIF Prolyl-Hydroxylase (1) Histone Demethylase (1) HSP (2) Interleukin Related (2) JAK (2) JNK (1) Microtubule/Tubulin (1) Mitochondrial Metabolism (1) mTOR (1) NF-κB (3) PI3K (3) PI5P4K (1) PROTACs (8) Reactive Oxygen Species (ROS) (2) Reference Standards (2) ROR (1) Src (1) STAT (3) Toll-like Receptor (TLR) (2) TrxR (1) VEGFR (1)
By Research Areas:	Cancer (66) Cardiovascular Disease (1) Inflammation/Immunology (2) Neurological Disease (1)
Click Chemistry:	Alkynes (1)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: Nuclear Factor of activated T Cells (NFAT) TREM receptor Programmed Cell Death 4 (PDCD4)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-144605

PROTAC EGFR degrader 3	EGFR PROTACs	Cancer
PROTAC EGFR degrader 3 is a potent PROTAC EGFR degrader. PROTAC EGFR degrader 3 shows excellent cellular activity against the H1975 and HCC827 cells with high selectively. PROTAC EGFR degrader 3 shows that the lysosome is involved in the degradation process of EGFR mutant degradation .

HY-123891

NS-062	EGFR	Cancer
NS-062 is an orally active, irreversible targeted covalent inhibitor for EGFR, and exhibits antiproliferative efficacy in drug-resistant double mutated H1975 cell with an IC₅₀ of 0.19 μM. NS-062 exhibits antitumor efficacy in mouse H1975 xenograft model .

HY-173038

EGFR-IN-151	EGFR ERK STAT Apoptosis	Cancer
EGFR-IN-151 (Compound 10) inhibits EGFR and its downstream signaling pathways ERK/STAT3. EGFR-IN-151 inhibits the proliferation of a variety lung cancer cells (IC₅₀s for NCI-H1781, HCC827, NCI-H3255 and NCI-H1975 is 11.7, 5.19, 7.32 and 1.53 μM, respectively), inhibits the colony formation and migration of H1975, arrests the cell cycle at G1 phase, and induces apoptosis in H1975 .

HY-146293

HDAC6/HSP90-IN-1	HDAC HSP	Cancer
HDAC6/HSP90-IN-1 (compound 17) is a potent and selective dual inhibitor of HDAC6 and HSP90, with IC₅₀ values of 4.3 and 46.8 nM, respectively. HDAC6/HSP90-IN-1 down-regulates PD-L1 expression in INF-γ treated H1975 lung cancer cells. HDAC6/HSP90-IN-1 inhibits tumor growth in human H1975 xenograft mice .

HY-170968

EGFR-IN-150	EGFR Apoptosis	Cancer
EGFR-IN-150 is an EGFR inhibitor that effectively suppresses the phosphorylation of mutant epidermal growth factor receptor (EGFR) and its downstream AKT signaling pathway, thereby exerting antitumor effects and inducing HMOX1 expression to trigger ferroptosis. EGFR-IN-150 exhibits an IC₅₀ of 0.386 μM against the non-small cell lung cancer (NSCLC) cell line H1975, and significantly inhibits colony formation and migration of both H1975 and A549 cells while inducing apoptosis. In addition, EGFR-IN-150 markedly suppresses tumor growth in the H1975 cell-derived xenograft (CDX) mouse model. EGFR-IN-150 holds promise for research related to non-small cell lung cancer .

HY-163396

EGFR-IN-107	EGFR Apoptosis	Cancer
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 .

HY-154960

Tubulin/AKT1-IN-1	Akt Apoptosis Microtubule/Tubulin	Cancer
Tubulin/AKT1-IN-1 (Compound D1-1) is an inhibitor of tubulin polymerization and AKT pathway activation. Tubulin/AKT1-IN-1 significantly inhibits the proliferation and metastasis of H1975 cells and slightly induced their apoptosis and can be used for non-small-cell lung cancer (NSCLC) research .

HY-156457

EGFR-IN-90	EGFR	Cancer
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 .

HY-157398

EGFR T790M/L858R-IN-3	EGFR	Cancer
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 .

HY-153043

DM-CO-(CH2)5-SMe	Drug Metabolite	Cancer
DM-CO-(CH2)5-SMe is an anticancer agent derived from antibody-drug conjugates (ADC) metabolite with cytotoxicity to H1703, H1975, COLO704 and Colo720E cells .

HY-171958

PROTAC EGFR degrader 12	PROTACs EGFR	Cancer
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 IC_{50_{s 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 .}}

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-147858A

PROTAC EGFR degrader 7 diTFA	PROTACs	Cancer
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 .

HY-164548

WK88-1	HSP Apoptosis	Cancer
WK88-1, a Hsp90 inhibitor, induces overall degradation of multiple oncogenic signaling molecules including EGFR, ErbB2 and ErbB3, leading to subsequent growth arrest and apoptosis in the Gefitinib-resistant H1975 cell line .

HY-147032

USP8-IN-1	Deubiquitinase	Cancer
USP8-IN-1 is a USP8 inhibitor with an IC₅₀ of 1.9 μM. USP8-IN-1 inhibits H1975 cell growth with a GI₅₀ of 82.04 μM (CN111138358A; U10) .

HY-164384

DFX117	PI3K Akt mTOR Apoptosis	Cancer
DFX117 is a selective, orally active inhibitor for PI3Kα and c-Met tyrosine kinase. DFX117 inhibits PI3K/Akt/mTOR pathway, inhibits the proliferation of NCI-H1975, NCI-H1993, and HCC827 with IC₅₀s 0.02-0.08 µM. DFX117 arrests cell cycle at G0/G1 phase, induces apoptosis in A549 and NCI-H1975. DFX117 exhibits antitumor efficacy in mice .

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-109061B

Lazertinib mesylate YH25448 mesylate; GNS-1480 mesylate	EGFR Akt ERK	Cancer
Lazertinib (mesylate) (YH25448 (mesylate); GNS-1480 (mesylate)) is an orally active EGFR inhibitor that can penetrate the blood-brain barrier. Lazertinib (mesylate) inhibits p-EGFR, p-AKT and p-ERK signaling pathways, leading to apoptosis. Lazertinib (mesylate) has anti-tumor activity in the mouse H1975-luc BM xenograft model. Lazertinib (mesylate) can be used in the study of non-small cell lung cancer .

HY-147862

EGFR-IN-62	EGFR Apoptosis	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/T790 M/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 .

HY-155227B

ALK/EGFR-IN-3	Anaplastic lymphoma kinase (ALK)	Cancer
ALK/EGFR-IN-3 is a dual inhibitor of ALK and EGFR. ALK/EGFR-IN-3 inhibits the cell proliferation of H1975, PC9, and Baf3-EML4-ALK cancer cell lines with IC₅₀s of 0.1360, 0.0332, and 0.0339 μM, respectively .

HY-147858

PROTAC EGFR degrader 7	PROTACs EGFR Apoptosis	Cancer
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.

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-146132

EGFR-IN-55	EGFR	Cancer
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 .

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-153901

PROTAC EGFR degrader 8	EGFR PROTACs	Cancer
PROTAC EGFR degrader 8 (T-184) is a PROTAC EGFR degrader. PROTAC EGFR degrader 8 degrades EGFR in HCC827 cell with a DC₅₀ of 15.56 nM. PROTAC EGFR degrader 8 inhibits H1975, PC-9, HCC827 cell growth with IC₅₀s of 7.72 nM, 121.9 nM, 14.21 nM. PROTAC EGFR degrader 8 can be used for research of cancer, especially NSCLC .

HY-155227A

ALK/EGFR-IN-2	Anaplastic lymphoma kinase (ALK)	Cancer
ALK/EGFR-IN-2 is a potent dual inhibitor of ALK and EGFR. ALK/EGFR-IN-2 induces apoptosis and G0/G1 cell cycle arrest in cancer cells. ALK/EGFR-IN-2 significantly inhibits the cell proliferation of H1975, PC9, and Baf3-EML4-ALK cancer cell lines with IC₅₀s of 0.0034, 0.0065, and 0.0018 μM, respectively .

HY-162640

LDR102	ROR	Cancer
LDR102 (Compound 19h) is an inhibitor for receptor tyrosine kinase-like orphan receptor 1 (ROR 1) with K_i of 0.10 μM. LDR102 inhibits proliferation of cancer cells H1975, A549 and MDA-MB-231, with IC₅₀ of 0.36 μM, 1.37 μM and 0.47 μM. LDR102 exhibits antitumor efficacy in mice and good pharmacokinetic characteristics in rat models .

HY-155203

Anticancer agent 154	Apoptosis Reactive Oxygen Species (ROS) Ferroptosis	Cancer
Anticancer agent 154 (Compound 8h) increases the levels of reactive oxygen species and leads to mitochondrial damage. Anticancer agent 154 induces cell apoptosis and DNA damage. Anticancer agent 154 also induces ferroptosis by reducing the GSH level and GPX4 expression and increasing the lipid peroxidation level. Anticancer agent 154 inhibits cancer cell (HT29, H1975, A549, and MCF-7) proliferation with IC₅₀s of 1.0-1.9 μM .

HY-101450

PF-6274484	EGFR	Cancer
PF-6274484 is a potent EGFR inhibitor with K_is 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 .

HY-146349

PROTAC EGFR degrader 4	PROTACs EGFR Autophagy	Cancer
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 .

HY-147860

EGFR-IN-61	EGFR	Cancer
EGFR-IN-61 (compound 22a) is a potent EGFR kinase inhibitor, with IC₅₀ values of 42 nM (L858R/T790 M), 137 nM (L858R/T790 M/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 .

HY-108016

Peruvoside Encordin	Src PI3K JNK STAT EGFR Apoptosis Autophagy	Cancer
Peruvoside is a potent inhibitor of Src, PI3K, JNK, STAT, and EGFR. Peruvoside induces apoptosis and autophagy and possesses a broad spectrum of anticancer activity in breast, lung, liver cancers and leukemia. Peruvoside is a broad-spectrum and potent antiviral activity against positive-sense RNA viruses. Peruvoside sensitizes Gefitinib (HY-50895)-resistant tumour cells (A549, PC9/gef and H1975) to Gefitinib .

HY-164056

EGFR T790M/L858R-IN-8	EGFR	Cancer
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 .

HY-161785

EGFR-IN-117	Apoptosis EGFR	Cancer
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 .

HY-170438

EGFR-IN-139	EGFR	Cancer
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].

HY-147826

EGFR-IN-60	EGFR Apoptosis	Cancer
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 .

HY-170927

JAK-IN-40	JAK STAT Apoptosis	Cancer
JAK-IN-40 (Compound 46) is the inhibitor for JAK that inhibits JAK1, JAK2 and JAK3 with IC₅₀s of 0.022, 0.759 and 1.601 μM, respectively. JAK-IN-40 inhibits the phosphorylation of STAT3. JAK-IN-40 inhibits the proliferation of cancer cell Ba/F3 and JAK1-TEL Ba/F3 with GI₅₀ of 0.614 μM and 0.193 μM. JAK-IN-40 arrests cell cycle of H1975 and H2087 at G2/M phase, induces apoptosis. JAK-IN-40 exhibits a synergistic antitumor effect with Osimertinib (HY-15772) .

HY-119396

DY3002	Endogenous Metabolite	Cancer
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 .

HY-155178

Antiproliferative agent-34	EGFR	Cancer
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 .

HY-151563A

OTUB1/USP8-IN-1 TFA	Deubiquitinase	Cancer
OTUB1/USP8-IN-1 TFA is the TFA salt form of OTUB1/USP8-IN-1 (HY-151563). OTUB1/USP8-IN-1 TFA is a dual inhibitor for OTUB1/USP8, IC₅₀ for OTUB1 and USP8 is 0.17 and 0.28 nM, respectively. OTUB1/USP8-IN-1 TFA inhibits proliferation of NSCLC cells. OTUB1/USP8-IN-1 TFA exhibits good pharmacokinetic characters in ICR mouse, and exhibits antitumor activity in H1975 xenograft mouse model .

HY-157432

EGFR-IN-97	EGFR Apoptosis	Cancer
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 .

HY-173007

ALK/PI3K/AKT-IN-1	Akt PI3K Anaplastic lymphoma kinase (ALK) CDK Apoptosis Mitochondrial Metabolism	Cancer
ALK/PI3K/AKT-IN-1 (Compound 45) inhibits the proliferation of cancer cell A549, H1975 and PC9 with an IC₅₀ of 0.44, 0.83 and 1.51 μM. ALK/PI3K/AKT-IN-1 increases the expression of p21 and p27, inhibits the activity of CDK2 and p-Rb, arrests the cell cycle at G1 phase. ALK/PI3K/AKT-IN-1 inhibits the ALK/PI3K/AKT signaling pathway, promotes the depolarization of mitochondrial membrane potential, and inducing apoptosis in A549 cell. ALK/PI3K/AKT-IN-1 inhibits the formation and growth of A549 cell spheroids .

HY-164392

TAS-121	EGFR Apoptosis	Cancer
TAS-121 is an orally active, selective, covalent, third-generation mutant EGFR-tyrosine kinase inhibitor (EGFR-TKI). TAS-121 inhibits the L858R mutation (IC₅₀=1.7 nM), Ex19del mutation (IC₅₀=2.7 nM), L858R/T790M mutation (IC₅₀=0.56 nM) and Ex19del/T790M mutation (IC₅₀=1.1 nM) and wild-type EGFR (IC₅₀=8.2 nM). TAS-121 inhibits HER2 and HER4 with IC₅₀s of 110 and 2.6 nM, respectively. TAS-121 inhibits phosphorylation of EGFR and its downstream signaling targets to block cell proliferation. TAS-121 induces apoptosis and displays antitumor activity in SW48 (EGFR G719S) and NCI-H1975 (EGFR L858R/T790M) xenograft models .

HY-116505

JAK1-IN-4	JAK	Cancer
JAK1-IN-4 is a potent and selective JAK1 inhibitor, with IC₅₀s of 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, and JAK3, respectively. JAK1-IN-4 inhibits STAT3 phosphorylation in NCI-H 1975 cells (IC₅₀, 227 nM) .

HY-151606

Akt3 degrader 1	Akt	Cancer
Akt3 degrader 1 (compound 12l) is a selective Akt3 degrader that overcomes Osimertinib (HY-15772)-induced resistance in H1975OR NSCLC cells. Akt3 degrader 1 also has anti-proliferative activity and significantly inhibits tumour growth in mice. Akt3 degrader 1 can be used in the study of drug-resistant non-small cell lung cancer .

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-149989

Ack1 inhibitor 1	Ack1 Akt	Cancer
Ack1 inhibitor 1 is a potent, selective, and orally active inhibitor of ACK1 kinase with an IC₅₀ value of 2.1 nM. Ack1 inhibitor 1 inhibits the phosphorylation of ACK1 and activation of downstream AKT. Ack1 inhibitor 1 has anti-tumor activity .

HY-174296

TMX-4102	PI5P4K	Others
TMX-4102 is a highly selective phosphatidylinositol 5-phosphate 4-kinase type II gamma (PIP4K2C) binder. TMX-4102 has binding activity to PIP4K2C (K_D = 0.45 nM) and has no significant effect on other lipid and non-lipid kinases.TMX-4102 specifically binds to PIP4K2C, regulating its scaffold function rather than its enzymatic activity. TMX-4102 can be used as a tool molecule to study the biological function and potential therapeutic value of PIP4K2C .

HY-18325A

AN-3485 hydrochloride	Toll-like Receptor (TLR) NF-κB Interleukin Related	Inflammation/Immunology Cancer
AN-3485 hydrochloride is a benzoxaborole analogue and an orally active antagonist of the Toll-like pathway. AN-3485 hydrochloride can inhibit TLR-mediated inflammatory cytokine secretion and has significant anti-inflammatory activity. In addition, AN-3485 hydrochloride also has certain anti-tumor activity .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-108016

Peruvoside Encordin	Apocynaceae Triterpenes Structural Classification Terpenoids Source classification Thevetia peruviana (Pers.) K. Schum. Plants	Src PI3K JNK STAT EGFR Apoptosis Autophagy
Peruvoside is a potent inhibitor of Src, PI3K, JNK, STAT, and EGFR. Peruvoside induces apoptosis and autophagy and possesses a broad spectrum of anticancer activity in breast, lung, liver cancers and leukemia. Peruvoside is a broad-spectrum and potent antiviral activity against positive-sense RNA viruses. Peruvoside sensitizes Gefitinib (HY-50895)-resistant tumour cells (A549, PC9/gef and H1975) to Gefitinib .

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 .

Cat. No.	Product Name		Classification

HY-147858

PROTAC EGFR degrader 7		Alkynes
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.

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