Signaling Pathway

EGFR

EGFR

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EGFR (The epidermal growth factor receptor; ErbB-1; HER1 in humans) is the cell-surface receptor for members of the epidermal growth factorfamily (EGF-family) of extracellular protein ligands. The epidermal growth factor receptor is a member of the ErbB family of receptors, a subfamily of four closely related receptor tyrosine kinases: EGFR (ErbB-1), HER2/c-neu (ErbB-2), Her 3 (ErbB-3) and Her 4 (ErbB-4). Mutations affecting EGFR expression or activity could result in cancer. EGFR exists on the cell surface and is activated by binding of its specificligands, including epidermal growth factor and transforming growth factor α (TGFα). EGFR dimerization stimulates its intrinsic intracellular protein-tyrosine kinase activity. As a result,autophosphorylation of several tyrosine (Y) residues in the C-terminal domain of EGFR occurs.

EGFR Inhibitors & Modulators (73)

Product Name Catalog No. Brief Description
AEE788

HY-10045

AEE788(NVP-AEE 788) is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2 nM and 6 nM, less potent to VEGFR2/KDR, c-Abl, c-Src, and Flt-1, does not inhibit Ins-R, IGF-1R, PKCα and CDK1.

Afatinib

HY-10261

Afatinib (BIBW2992) irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively; 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant.

Afatinib dimaleate

HY-10261A

Afatinib (BIBW2992) irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively; 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant.

AG 18

HY-15644

AG-18(RG-50810; Tyrphostin A23) inhibits EGFR with IC50 of 40 μM.

AG-1478

HY-13524

AG-1478 (NSC 693255) is a selective EGFR inhibitor with IC50 of 3 nM; almost no activity on HER2-Neu, PDGFR, Trk, Bcr-Abl and InsR.

AG-490

HY-12000

AG-490 (Tyrphostin AG 490) is an inhibitor of EGFR with IC50 of 0.1 μM, 135-fold more selective for EGFR versus ErbB2, also inhibits JAK2 with no activity to Lck, Lyn, Btk, Syk and Src.

Anlotinib

HY-19716

Anlotinib is a EGFR inhibitor extracted from patent 2015185012 A1, compound 1,which can be used to treat non-small cell lung cancer.

ARRY-380 analog

HY-10531

The product is the analog of ARRY-380, ARRY-380 is a potent and selective HER2 inhibitor with IC50 of 8 nM, equipotent against truncated p95-HER2, 500-fold more selective for HER2 versus EGFR

AST-1306

HY-15375

AST-1306 is a novel irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, also effective in mutation EGFR T790M/L858R, more potent to ErbB2-overexpressing cells, 3000-fold selective for ErbB family than other kinases.

AST-1306 TsOH

HY-13427

AST-1306 TsOH is a novel irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, also effective in mutation EGFR T790M/L858R, more potent to ErbB2-overexpressing cells, 3000-fold selective for ErbB family than other kinases.

AV-412

HY-10346

AV-412(MP-412, 2 tosylate salt) is a potent dual inhibitor of EGFR and ErbB2(IC50=19 nM) tyrosine kinases, including the mutant EGFR(L858R IC50=0.51 nM, T790M IC50=0.79 nM); inhibits autophosphorylation of EGFR and ErbB2 with IC(50) of 43 and 282 nM, respectively.

AV-412 free base

HY-10346A

AV-412(MP-412) is a potent dual inhibitor of EGFR and ErbB2(IC50=19 nM) tyrosine kinases, including the mutant EGFR(L858R IC50=0.51 nM, T790M IC50=0.79 nM); inhibits autophosphorylation of EGFR and ErbB2 with IC(50) of 43 and 282 nM, respectively.

AZ-5104

HY-B0793

AZ-5104 is a potent EGFR inhibitor, displays potent antitumor activities both in vitro and in vivo.

AZD-9291

HY-15772

AZD-9291 is a potent and selective mutated forms EGFR inhibitor(Exon 19 deletion EGFR IC50=12.92 nM, L858R/T790M EGFR IC50= 11.44 nM, wild type EGFR IC50= 493.8 nM).

AZD-9291 dimesylate

HY-79077

AZD-9291 dimesylate is a potent and selective mutated forms EGFR inhibitor(Exon 19 deletion EGFR IC50=12.92 nM, L858R/T790M EGFR IC50= 11.44 nM, wild type EGFR IC50= 493.8 nM).

AZD-9291 mesylate

HY-15772A

AZD-9291 is a potent and selective mutated forms EGFR inhibitor(Exon 19 deletion EGFR IC50=12.92 nM, L858R/T790M EGFR IC50= 11.44 nM, wild type EGFR IC50= 493.8 nM).

AZD3759

HY-18750

AZD3759 is a potent, oral active, central nervous system-penetrant, EGFR inhibitor.

BIBX 1382

HY-10322

BIBX 1382 is a potent, selective inhibitor of EGFR tyrosine kinase (IC50 = 3 nM); displays > 1000-fold lower potency against ErbB2 (IC50 = 3.4 μM) and a range of other related tyrosine kinases (IC50 > 10 μM).

BMS-599626

HY-10251

AC480 (BMS-599626) is a selective and efficacious inhibitor of HER1 and HER2 with IC50 of 20 nM and 30 nM, ~8-fold less potent to HER4, >100-fold to VEGFR2, c-Kit, Lck, MET etc.

BMS-599626 Hydrochloride

HY-12010

AC480 (BMS-599626) is a selective and efficacious inhibitor of HER1 and HER2 with IC50 of 20 nM and 30 nM, ~8-fold less potent to HER4, >100-fold to VEGFR2, c-Kit, Lck, MET etc.