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Isoforms Recommended:	EGFR/ErbB1/HER1

Results for "

EGFR(T790M)

" in MedChemExpress (MCE) Product Catalog:

By Targets:	EGFR (34) Apoptosis (10) Bcl-2 Family (1) BMX Kinase (1) Btk (3) c-Met/HGFR (1) Caspase (1) CDK (1) Discoidin Domain Receptor (1) Isotope-Labeled Compounds (1) JNK (1) MEK (1) p38 MAPK (1) Raf (1)
By Research Areas:	Cancer (34) 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-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 is a potent EGFR ^T790M/L858R inhibitor with anticancer effects (WO2024064091A1; Example 14) .

EGFR T790M/L858R-IN-4	EGFR	Cancer
EGFR T790M/L858R-IN-4 is a potent EGFR ^T790M/L858R inhibitor with anticancer effects (WO2024064091A1; Example 14) .

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-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.

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

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 .

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-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 2 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 2 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 2 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 2 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-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-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 5+ Cited Publications 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-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) .

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.

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.

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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