EGFR/ErbB1 Selective Inhibitors

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S1079 PD153035 HCl

PD153035 HCl is a potent and specific inhibitor of EGFR with Ki and IC50 of 5.2 pM and 29 pM in cell-free assays; little effect noted against PGDFR, FGFR, CSF-1, InsR and Src.

Selective EGFR, Ki: 5.2 pM; EGFR, Ki: 5.2 pM
S7557 CL-387785 (EKI-785)

CL-387785 (EKI-785) is an irreversible, and selective EGFR inhibitor with IC50 of 370 pM.

Selective EGFR, IC50: 370 pM
S7039 PD168393

PD168393 is an irreversible EGFR inhibitor with IC50 of 0.70 nM, irreversibly alkylate Cys-773; inactive against insulin, PDGFR, FGFR and PKC.

Selective EGFR, IC50: 0.70 nM
S2205 OSI-420

OSI-420 is the active metabolite of Erlotinib (EGFR inhibitor with IC50 of 2 nM).

Selective EGFR, IC50: 2 nM
S7786 Erlotinib

Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.

Selective EGFR, IC50: 2 nM
S1023 Erlotinib HCl (OSI-744)

Erlotinib HCl (OSI-744) is an EGFR inhibitor with IC50 of 2 nM in cell-free assays, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.

Selective HER1/EGFR, IC50: 2 nM
S1173 WZ4002

WZ4002 is a novel, mutant-selective EGFR inhibitor for EGFR(L858R)/(T790M) with IC50 of 2 nM/8 nM in BaF3 cell line; does not inhibit ERBB2 phosphorylation (T798I).

Selective EGFR (L858R), IC50: 2 nM; EGFR (L858R/T790M), IC50: 8 nM
S1170 WZ3146

WZ3146 is a mutant-selective irreversible inhibitor of EGFR(L858R) and EGFR(E746_A750) with IC50 of 2 nM and 2 nM; does not inhibit ERBB2 phosphorylation (T798I).

Selective EGFR (E746_A750/T790M), IC50: 14 nM; EGFR (L858R/T790M), IC50: 5 nM; EGFR (E746_A750), IC50: 2 nM; EGFR (L858R), IC50: 2 nM
S2728 AG-1478 (Tyrphostin AG-1478)

AG-1478 (Tyrphostin AG-1478) is a selective EGFR inhibitor with IC50 of 3 nM in cell-free assays, almost no activity on HER2-Neu, PDGFR, Trk, Bcr-Abl and InsR.

Selective EGFR, IC50: 3 nM
S2867 WHI-P154

WHI-P154 is a potent JAK3 inhibitor with IC50 of 1.8 μM, no activity against JAK1 or JAK2, also inhibits EGFR, Src, Abl, VEGFR and MAPK, prevents Stat3, but not Stat5 phosphorylation.

Selective EGFR, IC50: 4 nM
S2922 Icotinib

Icotinib is a potent and specific EGFR inhibitor with IC50 of 5 nM, including the EGFR, EGFR(L858R), EGFR(L861Q), EGFR(T790M) and EGFR(T790M, L858R).

Selective EGFR, IC50: 5 nM
S7297 AZD9291

AZD9291 is an oral, irreversible, and mutant-selective EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR in LoVo cells, respectively. Phase 3.

Selective WT EGFR, IC50: 493.8 nM; L858R/T790M EGFR, IC50: 11.44 nM; Exon 19 deletion EGFR, IC50: 12.92 nM
S7206 CNX-2006

CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR.

Selective mutant EGFR, IC50: <20 nM
S7284 Rociletinib (CO-1686, AVL-301)

Rociletinib (CO-1686, AVL-301) is an irreversible, mutant-selective EGFR inhibitor with Ki of 21.5 nM and 303.3 nM for EGFRL858R/T790M and EGFRWT in cell-free assays, respectively. Phase 2.

Selective EGFR (L858R/T790M), Ki: 21.5 nM; EGFR (wt), Ki: 303.3 nM
S1025 Gefitinib (ZD1839)

Gefitinib (ZD-1839) is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively.

Selective Tyr992 (NR6W cells), IC50: 57 nM; Tyr1173 (NR6W cells), IC50: 26 nM; Tyr1173 (NR6wtEGFR cells), IC50: 37 nM; Tyr992 (NR6wtEGFR cells), IC50: 37 nM
S1392 Pelitinib (EKB-569)

Pelitinib (EKB-569) is a potent irreversible EGFR inhibitor with IC50 of 38.5 nM. Phase2.

Selective EGFR, IC50: 38.5 nM
S1143 AG-490 (Tyrphostin B42)

AG-490 (Tyrphostin B42) is an inhibitor of EGFR with IC50 of 0.1 μM in cell-free assays, 135-fold more selective for EGFR versus ErbB2, also inhibits JAK2 with no activity to Lck, Lyn, Btk, Syk and Src.

Selective EGFR, IC50: 0.1 μM
S8009 AG-18

AG-18 inhibits EGFR with IC50 of 35 μM.

Selective EGFR, IC50: 35 μM
S2895 Tyrphostin 9

Tyrphostin 9 is firstly designed as an EGFR inhibitor with IC50 of 460 μM, but is also found to be more potent to PDGFR with IC50 of 0.5 μM.

Selective EGFR, IC50: 460 μM
S8036 Butein

Butein, a plant polyphenol isolated from Rhus verniciflua, is able to inhibit the activation of protein tyrosine kinase, NF-κB and STAT3, also inhibits EGFR

Selective
S1179 WZ8040

WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I).

Selective
S1342 Genistein

Genistein, a phytoestrogen found in soy products, is a highly specific inhibitor of protein tyrosine kinase (PTK) which blocks the mitogenic effect mediated by EGF on NIH-3T3 cells with IC50 of 12μM or by insulin with IC50 of 19 μM.

Selective
S2406 Chrysophanic Acid

Chrysophanic acid (Chrysophanol), a natural anthraquinone isolated from Dianella longifolia, is a EGFR/mTOR pathway inhibitor.

Selective
S1011 Afatinib (BIBW2992)

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 in cell-free assays, respectively; 100-fold more active against Gefitinib-res

Pan EGFR (L858R/T790M), IC50: 10 nM; EGFR (L858R), IC50: 0.4 nM; EGFR (wt), IC50: 0.5 nM
S7810 Afatinib (BIBW2992) Dimaleate

Afatinib (BIBW2992) Dimaleate 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.

Pan EGFR (wt), IC50: 0.5 nM; EGFR (L858R/T790M), IC50: 10 nM; EGFR (L858R), IC50: 0.4 nM
S2185 AST-1306

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,

Pan EGFR, IC50: 0.5 nM; EGFR (T790M/L858R), IC50: 12 nM
S1019 Canertinib (CI-1033)

Canertinib (CI-1033) is a pan-ErbB inhibitor for EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM, no activity to PDGFR, FGFR, InsR, PKC, or CDK1/2/4. Phase 3.

Pan EGFR, IC50: 1.5 nM
S1486 AEE788 (NVP-AEE788)

AEE788 (NVP-AEE788) 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. Phase 1/2.

Pan EGFR, IC50: 2 nM
S1194 CUDC-101

CUDC-101 is a potent multi-targeted inhibitor against HDAC, EGFR and HER2 with IC50 of 4.4 nM, 2.4 nM, and 15.7 nM, and inhibits class I/II HDACs, but not class III, Sir-type HDACs. Phase 1.

Pan EGFR, IC50: 2.4 nM
S7358 Poziotinib (HM781-36B)

Poziotinib (HM781-36B) is an irreversible pan-HER inhibitor with IC50 of 3.2 nM, 5.3 nM and 23.5 nM for HER1, HER2, and HER4, respectively. Phase 2.

Pan HER1, IC50: 3.2 nM
S2192 AZD8931 (Sapitinib)

AZD8931 (Sapitinib) is a reversible, ATP competitive inhibitor of EGFR, ErbB2 and ErbB3 with IC50 of 4 nM, 3 nM and 4 nM in cell-free assays, more potent than Gefitinib or Lapatinib against NSCLC cell, 100-fold more selective f

Pan EGFR, IC50: 4 nM
S2727 Dacomitinib (PF299804, PF299)

Dacomitinib (PF299804, PF299) is a potent, irreversible pan-ErbB inhibitor, mostly to EGFR with IC50 of 6 nM in a cell-free assay, effective against NSCLCs with EGFR or ERBB2 mutations (resistant to gefitinib) as well as those harboring the

Pan EGFR, IC50: 6.0 nM
S2755 Varlitinib

Varlitinib is a selective and potent ErbB1(EGFR) and ErbB2(HER2) inhibitor with IC50 of 7 nM and 2 nM, respectively. Phase 2.

Pan ErbB1, IC50: 7 nM
S2111 Lapatinib

Lapatinib, used in the form of Lapatinib Ditosylate, is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively.

Pan EGFR, IC50: 10.8 nM
S1028 Lapatinib (GW-572016) Ditosylate

Lapatinib (GW-572016) Ditosylate is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively.

Pan EGFR, IC50: 10.8 nM
S1056 AC480 (BMS-599626)

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. Phase 1.

Pan HER1, IC50: 20 nM
S2784 TAK-285

TAK-285 is a novel dual HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, >10-fold selectivity for HER1/2 than HER4, less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. Phase 1.

Pan EGFR/HER1, IC50: 23 nM
S2150 Neratinib (HKI-272)

Neratinib (HKI-272) is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM in cell-free assays; weakly inhibits KDR and Src, no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf and c-Met. Phase 3.

Pan EGFR, IC50: 92 nM