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Isoforms Recommended:	EGFR/ErbB1/HER1

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EGFR-T790M

" in MedChemExpress (MCE) Product Catalog:

By Targets:	EGFR (41) Apoptosis (10) Bcl-2 Family (1) BMX Kinase (1) Btk (3) c-Met/HGFR (1) Caspase (1) CDK (1) Discoidin Domain Receptor (1) Endogenous Metabolite (1) GSK-3 (1) Isotope-Labeled Compounds (1) JAK (1) JNK (1) MEK (1) p38 MAPK (1) PD-1/PD-L1 (1) Raf (1)
By Research Areas:	Cancer (42) Inflammation/Immunology (1)
Click Chemistry:	Alkynes (2)

Inhibitors & Agonists

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: EGFR

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-149824

EGFR T790M/L858R-IN-2	EGFR Apoptosis	Cancer
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 .

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 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-156912

Tyrosine kinase-IN-7	EGFR	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 .

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-158178

EGFR T790M/L858R-IN-7	EGFR	Cancer
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 .

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-158175

EGFR T790M/L858R-IN-4	EGFR	Cancer
EGFR T790M/L858R-IN-4 (Example 14) is a potent EGFR ^T790M/L858R inhibitor with anticancer effects .

HY-158177

EGFR T790M/L858R-IN-6	EGFR	Cancer
EGFR T790M/L858R-IN-6 (compound 53), a pyrimidine compound, is a potent **EGFR T790M/L858R** inhibitor. EGFR T790M/L858R-IN-6 shows 90.88% enzyme activity inhibition with 0.05 μM .

HY-158176

EGFR T790M/L858R-IN-5	EGFR	Cancer
EGFR T790M/L858R-IN-5 (example 52) is a potent inhibitor of *EGFR* T790M/L858R with the inhibition percentage of 92.9% in the concerntration of 0.05 μM .

HY-164476

ES-072	EGFR GSK-3 PD-1/PD-L1	Cancer
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 .

HY-12029

WZ8040	EGFR	Cancer
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 .

HY-13984

*Mutant EGFR* inhibitor**	EGFR	Cancer
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.

HY-153111

EGFR/HER2-IN-9	EGFR	Cancer
EGFR/HER2-IN-9 (Compound 1) is an *EGFR* and HER2 inhibitor with IC₅₀s of 3.2, 8.3 and 14 nM against EGFR, EGFR T790M and HER2, respectively .

HY-161045

T-1-DOCA	EGFR Apoptosis	Cancer
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 .

HY-138751A

limertinib diTFA ASK120067 diTFA	EGFR	Cancer
limertinib (ASK120067) diTFA is a potent and orally active inhibitor of *EGFR ^T790M* (IC₅₀: 0.3 nM) with selectivity over *EGFR* ^WT (IC₅₀: 6.0 nM). limertinib diTFA is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC) .

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-138627B

AST5902 mesylate	Others	Cancer
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.

HY-138751

limertinib ASK120067	EGFR	Cancer
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) .

HY-146782

EGFR-IN-49	EGFR	Cancer
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 .

HY-150552

JNK3 inhibitor-2	JNK Discoidin Domain Receptor	Inflammation/Immunology Cancer
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 .

HY-10346

AV-412 4 Publications Verification MP412	EGFR	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.

HY-100213

EAI045 1 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-10346A

AV-412 free base 4 Publications Verification MP-412 free base	EGFR	Cancer
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.

HY-146136

EGFR-IN-56	EGFR Apoptosis	Cancer
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 .

HY-155537

YK-029A	EGFR	Cancer
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 .

HY-161067

EGFR-IN-96	EGFR Apoptosis	Cancer
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 .

HY-162360

EGFR-IN-109	Apoptosis EGFR Caspase Bcl-2 Family	Cancer
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 .

HY-19816A

Avitinib maleate 3 Publications Verification Abivertinib maleate; AC0010 maleate	EGFR Btk Apoptosis	Cancer
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 .

HY-19816

Avitinib 3 Publications Verification Abivertinib; AC0010	EGFR Btk Apoptosis	Cancer
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 .

HY-15164

Icotinib Hydrochloride Maximum Cited Publications 8 Publications Verification BPI-2009H	EGFR	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.

HY-15164A

Icotinib Maximum Cited Publications 8 Publications Verification BPI-2009	EGFR	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.

HY-W740378

1,2,3,4-Tetrahydro Staurosporin AFN-941	EGFR JAK	Others
1,2,3,4-Tetrahydrostaurosporine is a derivative of Staurosporine (HY-15141) and an inhibitor of mutant EGFR (IC₅₀=74 nM for EGFRT790M). It is selective for EGFRT790M over wild-type EGFR (IC₅₀=390 nM). It also binds to Janus kinase 3 (JAK3).

HY-146210

EGFR-IN-50	EGFR	Cancer
EGFR-IN-50 (Compound 9h) is a potent *EGFR* inhibitor against L858R resistance mutation (TEL-EGFR-L858R-BaF3: GI₅₀=8 nM, TEL-EGFR-T790M-L858R-BaF3: GI₅₀=6.03 μM). EGFR-IN-50 shows anti-proliferative activity to cancer cells .

HY-152098

HX103	EGFR	Cancer
HX103 is an epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitor (TKI)-based fluorogenic probe. HX103 inhibits EGFR 19 del, EGFR L858R, EGFR wild type and *EGFR T790M* with IC₅₀s of 1.3, 1.5, 4.0 and 977 nM, respectively. HX103 can be used for quantifying active-EGFR to predict agent sensitivity in NSCLC patients with EGFR-activating mutations .

HY-162062

EGFR WT/T790M/L858R-IN-1	EGFR	Cancer
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 .

HY-15164AR

Icotinib (Standard)	EGFR	Cancer
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.

HY-15164AS

Icotinib-d4 BPI-2009-d₄	Isotope-Labeled Compounds	Others
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.

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-15730

Poziotinib Maximum Cited Publications 8 Publications Verification HM781-36B; NOV120101	EGFR Apoptosis	Cancer
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 .

HY-164503

Neptinib NEP010	EGFR	Cancer
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 *EGFR* ^wt, *EGFR* ^L858R/T790M, *EGFR* ^L858R and *EGFR* ^T790M, respectively .

HY-149518

EGFR/BRAFV600E-IN-3	EGFR Apoptosis	Others
EGFR/BRAFV600E-IN-3 is a *EGFR, BRAFV600E* and *EGFRT790M* inhibitor with IC₅₀ value of 57 nM, 68 nM and 9.70 nM. EGFR/BRAFV600E-IN-3 is an apoptotic inducer and also displays promising antioxidant activity .

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 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 .

HY-155736

MAPK-IN-2	p38 MAPK EGFR Raf CDK c-Met/HGFR	Cancer
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 ^WT IC₅₀=281 nM, c-MET IC₅₀=205 nM, B-RAF ^WT IC₅₀=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 ^T790M IC₅₀=69 nM and B-RAF ^V600E IC₅₀=83 nM) .

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-139920

Oritinib SH-1028	EGFR	Cancer
Oritinib (SH-1028), an irreversible third-generation EGFR TKI, overcomes T790M-mediated resistance in non-small cell lung cancer. Oritinib (SH-1028), a mutant-selective inhibitor of EGFR kinase activity, inhibits EGFR ^WT, EGFR ^L858R, EGFR ^L861Q, EGFR ^L858R/T790M, EGFR ^d746-750 and EGFR ^{d746-750/T790M} kinases, with IC₅₀s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM, respectively .

Cat. No.	Product Name	Chemical Structure

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-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-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.

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