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Isoforms Recommended:	EGFR/ErbB1/HER1

Results for "

EGFR WT

" in MedChemExpress (MCE) Product Catalog:

By Targets:	EGFR (57) Akt (4) Apoptosis (17) Autophagy (4) Bcl-2 Family (1) BMX Kinase (1) Btk (2) c-Met/HGFR (5) Caspase (1) CDK (1) ERK (1) MEK (1) p38 MAPK (4) Potassium Channel (1) PROTACs (4) Raf (2) Src (1) VEGFR (1)
By Research Areas:	Cancer (58) Inflammation/Immunology (1)

Targets Recommended: EGFR

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-150611

EGFR-IN-70	EGFR	Cancer
EGFR-IN-70 (compound 18j) is a potent *EGFR* inhibitor with IC₅₀ values of 23.6 and 307.5 nM for EGFR ^LR/TM/CS and EGFR ^WT, respectively. EGFR-IN-70 has anti-proliferative activity and suppresses phosphorylation of the EGFR. EGFR-IN-70 can be used for cancer research .

HY-147941A

MS9427 TFA	PROTACs EGFR	Cancer
MS9427 TFA is a potent PROTAC EGFR degrader with K_ds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 TFA selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 TFA potently inhibits the proliferation of NSCLC cells. MS9427 TFA can be used for researching anticancer .

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-163371

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

HY-157994

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

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-144053

EGFR-IN-36	EGFR	Cancer
EGFR-IN-36 is a potent *EGFR* inhibitor with IC₅₀s of 19.09 nM, 120.01 nM, 2.35 nM for EGFR (WT), HER2 (WT), HER2 (A775_G776insYVMA), respectively. EGFR-IN-36 has potential for wild and/or mutant EGFR and/or HER2 kinase mediated tumors research .

HY-147941

MS9427	PROTACs EGFR	Cancer
MS9427 is a potent PROTAC EGFR degrader with K_ds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 potently inhibits the proliferation of NSCLC cells. MS9427 can be used for researching anticancer .

HY-152144

EGFR-IN-75	EGFR	Cancer
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 .

HY-162623

EGFR/HER2-IN-15	EGFR	Cancer
EGFR/HER2-IN-15, a dihydropyrimidine, is a potent *EGFR/HER2* inhibitor. EGFR/HER2-IN-15 significantly inhibits EGFR ^wt activity with an IC₅₀ of 37.21 nM. EGFR/HER2-IN-15 has anticaner effects .

HY-158149

T-1-PMPA	EGFR Apoptosis	Cancer
T-1-PMPA is a potent *EGFR* inhibitor with apoptotic properties. T-1-PMPA effectively inhibits EGFR ^WT and EGFR ^790m, with IC₅₀ values of 86 nM and 561.73 nM, respectively .

HY-19815

Olafertinib	EGFR	Cancer
Olafertinib is a third-generation *EGFR* TKI, with GI₅₀ values of 5 nM (EGFR L858R/T790M), 10 nM (EGFR del19) and 689 nM (EGFR WT), respectively. Olafertinib has the potential for NSCLC research .

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-156741

EGFR-IN-87	EGFR	Cancer
EGFR-IN-87 is a *EGFR* tyrosine kinase inhibitor. EGFR-IN-87 has IC₅₀ value of 3.1 nM, 1.3 nM and 7.1 nM for EGFR_d746-750, EGFR_L858R/T790 and EGFR_WT in A431 cells, respectively. EGFR-IN-87 can be used for cancer diseases research .

HY-144044

EGFR-IN-30	EGFR	Cancer
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 .

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-141640

MS154	PROTACs EGFR	Cancer
MS154 is a first-in-class E3 ligase cereblon-recruiting *EGFR* degrader with K_ds of 1.8 nM and 3.8 nM for EGFR ^WT and EGFR ^L858R mutants. MS154 potently inhibits cell proliferation in lung cancer cells .

HY-133780

Afatinib impurity 11	EGFR Autophagy	Cancer
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 .

HY-142517

EGFR-IN-25	EGFR	Cancer
EGFR-IN-25 is a potent *EGFR* inhibitor with IC₅₀s of 9 nM and 60 nM for BaF3 cells (EGFR DEL19/T790M/C797S) and A431 cells (WT), 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-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-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-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-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-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-147942

MS9449	PROTACs EGFR	Cancer
MS9449 is a potent PROTAC EGFR degrader with K_ds of 17 nM and 10 nM for EGFR WT and EGFR L858R, respectively. MS9449 effectively induces degradation of mutant EGFRs through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9449 potently inhibits the proliferation of NSCLC cells. MS9449 can be used for researching anticancer .

HY-155118

EGFR-IN-81	EGFR	Cancer
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 .

HY-128778

DBPR112	EGFR	Cancer
DBPR112 is an orally active furanopyrimidine-based *EGFR* inhibitor with IC₅₀s of 15 nM and 48 nM for EGFR ^WT and EGFR ^L858R/T790M, respectively. DBPR112 can occupy the ATP-binding site. DBPR112 has significant antitumor efficacy .

HY-18750A

Zorifertinib hydrochloride AZD3759 hydrochloride	EGFR Apoptosis	Cancer
Zorifertinib (AZD3759) hydrochloride is a potent, orally active, central nervous system-penetrant, *EGFR* inhibitor (IC₅₀s: 0.3, 0.2, and 0.2 nM for EGFR ^wt, EGFR ^L858R, and EGFR ^{exon 19Del}, respectively). Zorifertinib hydrochloride induces cancer cell apoptosis. Zorifertinib hydrochloride has antitumor activity, and can be used for NSCLC, HCC etc. 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-18750

Zorifertinib 5+ Cited Publications AZD3759	EGFR Apoptosis	Cancer
Zorifertinib (AZD3759) is a potent, orally active, central nervous system-penetrant, *EGFR* inhibitor. At K_m ATP concentrations, the IC₅₀s are 0.3, 0.2, and 0.2 nM for EGFR ^wt, EGFR ^L858R, and EGFR ^{exon 19Del}, respectively. Zorifertinib induces cancer cell apoptosis. Zorifertinib has antitumor activity, and can be used for NSCLC, HCC etc. research .

HY-143319

SPH5030	Others	Cancer
SPH5030 is a selective and irreversible HER2 inhibitor. SPH5030 inhibits HER2 ^WT and EGFR ^WT with IC₅₀s of 3.51 and 8.13 nM, respectively. SPH5030 shows excellent activities against HER2 mutants. SPH5030 can be used for the research of cancer .

HY-132842

Sunvozertinib 1 Publications Verification DZD9008	EGFR Btk	Cancer
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) .

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-143445

EGFR-IN-48	EGFR	Cancer
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 .

HY-149401

EGFR-IN-82	EGFR	Cancer
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 .

HY-162299

EGFR kinase inhibitor 3	EGFR	Cancer
EGFR kinase inhibitor 3 (compound 2) is a bivalent ATP-allosteric *EGFR* kinase inhibitor with IC₅₀s of <10 nM, 1.5 nM, 0.059 nM, 0.064 nM for WT EGFR, EGFR-activating mutations L858R, L858R/T790M and L858R/T790M/C797S, respectively. EGFR kinase inhibitor 3 is a C-linked inhibitor .

HY-161923

EGFR-IN-120	EGFR Apoptosis Akt ERK	Cancer
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 .

HY-153557

HER2-IN-13	EGFR Potassium Channel	Cancer
HER2-IN-13 (Compound 33) is an HER2 inhibitor with an IC₅₀ of 8 nM. HER2-IN-13 also inhibits *wt-EGFR* with an IC₅₀ of 0.40 μM .

HY-153557A

HER2-IN-14	EGFR	Cancer
HER2-IN-14 (Compound 34) is an HER2 inhibitor with an IC₅₀ of 18 nM. HER2-IN-14 also inhibits *wt-EGFR* with an IC₅₀ of 6.3 μM .

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 .

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-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-10261

Afatinib Maximum Cited Publications 60 Publications Verification BIBW 2992	EGFR Autophagy Apoptosis c-Met/HGFR Akt p38 MAPK	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 .

HY-10261A

Afatinib dimaleate Maximum Cited Publications 60 Publications Verification BIBW 2992MA2	EGFR Autophagy Apoptosis c-Met/HGFR Akt p38 MAPK	Cancer
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 .

HY-10261D

Afatinib oxalate BIBW 2992 oxalate	EGFR Autophagy Apoptosis c-Met/HGFR Akt	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 .

HY-143246

EGFR kinase inhibitor 1	EGFR Apoptosis	Cancer
EGFR kinase inhibitor 1 is a potent *EGFR* inhibitor with IC₅₀s of 37, 1.7, >300 nM for WT, l885R/T790M, L858R/T790M/C797S, respectively. EGFR kinase inhibitor 1 induces apoptosis and cell cycle arrest at G0/G1-phase. EGFR kinase inhibitor 1 inhibits the cell motility. EGFR kinase inhibitor 1 shows antiproliferative and anti-tumor activity .

HY-119944

JND3229 1 Publications Verification	EGFR	Cancer
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 .

HY-163428

ZN-A-1041	EGFR	Inflammation/Immunology Cancer
ZN-A-1041 inhibits HER2 in BT474 cell and *wt-EGFR* in H838 cells, with IC₅₀s of 9.5 nM and 12 μM respectively. ZN-A-1041 can be used for research of cancer and inflammation .

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 .

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