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EGFR Inhibitors (39)


Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1023 Erlotinib HCl (OSI-744) Erlotinib HCl (OSI-744) is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.
  • Cell, 2012, 151(5):937-50
  • Nat Genet, 2012, 44(8):852-60
  • Cell Metab, 2013, 17(6):1000-8
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.
  • Nature, 2014, 508(7494):118-22
  • Nature, 2012, 483(7387):100-3
  • Cell, 2012, 151(5):937-50
S1028 Lapatinib (GW-572016) Ditosylate Lapatinib Ditosylate (GW572016, GW2016) is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM, respectively.
  • Nat Commun, 2014, 5:3384
  • Proc Natl Acad Sci U S A, 2012, 109(17):6584-9
  • Oncogene, 2012, 32(37):4331-42
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, respectively; 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant.
  • Cancer Discov, 2013, 3(2):168-81
  • Nat Commun, 2014, 5:5232
  • Cancer Research, 2014, 74(1):341-52
S2150 Neratinib (HKI-272) Neratinib (HKI-272) is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM; 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.
  • Cancer Discov, 2013, 3(2):168-81
  • Cancer Discov, 2013, 3(2):224-37
  • Cancer Discov, 2012, 2(5):458-71
S7557 CL-387785 (EKI-785) CL-387785 (EKI-785) is an irreversible, and selective EGFR inhibitor with IC50 of 370 pM.
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.
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.
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, respectively. Phase 3.
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.
  • Cancer Discov, 2012, 2(5):458-71
  • J Cell Sci, 2010, 123(Pt 18):3102-11
  • Carcinogenesis, 2010, 31(11):1948-55
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, respectively.
  • Cancer Cell, 2012, 21(4):488-503
  • ACS Nano, 2012, 6(10):8525-35
  • Proc Natl Acad Sci U S A, 2014, 109(17):6584-9
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.
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.
S8009 AG-18 AG-18 inhibits EGFR with IC50 of 35 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
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, respectively. Phase 2.
  • J Thorac Oncol, 2015, 10.1097/JTO.0000000000000500
S1173 WZ4002 WZ4002 is a novel, mutant-selective EGFR inhibitor for EGFR(L858R)/(T790M) with IC50 of 2 nM/8 nM; does not inhibit ERBB2 phosphorylation (T798I).
  • Proc Natl Acad Sci U S A, 2013, 110(38):E3595-604
  • Oncogene, 2013, 32(37):4427-35
  • Clin Cancer Res, 2012, 18(6):1663-71
S1392 Pelitinib (EKB-569) Pelitinib (EKB-569) is a potent irreversible EGFR inhibitor with IC50 of 38.5 nM. Phase2.
  • J Immunol, 2012, 188(9):4581-9
  • Infect Immun, 2014, 82(3):1243-55
  • Drug Metab Dispos, 2014, 42(11):1851-7
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.
  • Cancer Cell, 2012, 22(5):656-67
  • Genes Cancer, 2014, 5(7-8):261-72
  • J Cell Mol Med, 2013, 17(5):648-56
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.
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.
  • J Chem Inf Model, 2014, 54(3):881-93
  • ACS Med Chem Lett, 2013, 4(9):858-62
  • Bioorganic & Medicinal Chemistry, 10.1016/j.bmc.2014.12.066,
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.
  • Prostate, 2013, 73(13):1453-61
S2406 Chrysophanic Acid Chrysophanic acid (Chrysophanol), a natural anthraquinone isolated from Dianella longifolia, is a EGFR/mTOR pathway inhibitor.
S1167 CP-724714 CP-724,714 is a potent, selective inhibitor of HER2/ErbB2 with IC50 of 10 nM, >640-fold selectivity against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met etc. Phase 2.
  • Cancer Res, 2014, 74(1):341-52
  • Cell Death Dis, 2014, 5:e1194
  • Exp Cell Res, 332(2):223-35,
S2727 Dacomitinib (PF299804, PF299) PF-299804 is a potent, irreversible pan-ErbB inhibitor, mostly to EGFR with IC50 of 6 nM, effective against NSCLCs with EGFR or ERBB2 mutations (resistant to gefitinib) as well as those harboring the EGFR T790M mutation. Phase 2.
  • J Immunol, 2013, 192(2):722-31
  • Cell Cycle, 14(4):648-55,
  • J Gastrointest Surg, 2013, 17(10):1723-31
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.
S1143 AG-490 (Tyrphostin B42) AG-490 (Tyrphostin B42) 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.
  • Clin Cancer Res, 2013, 19(17):4697-705
  • Mol Cancer, 2014, 13:176
  • Carcinogenesis, 2015, 36(1):142-50
S2728 AG-1478 (Tyrphostin AG-1478) AG-1478 (Tyrphostin AG-1478) is a selective EGFR inhibitor with IC50 of 3 nM, almost no activity on HER2-Neu, PDGFR, Trk, Bcr-Abl and InsR.
  • Cell Rep, 2013, 4(4):764-75
  • J Pharmacol Exp Ther, 2012, 341(2):386-95
  • PLoS One, 2013, 8(8): e70353
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,
  • Cancer Lett, 2014, 350(1-2):61-8
S2752 HER2-Inhibitor-1 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. Phase 1.
S2205 OSI-420 OSI-420 is the active metabolite of Erlotinib (EGFR inhibitor with IC50 of 2 nM).
  • Carcinogenesis, 2010, 31(11), 1948-1955
  • Sci Pharm, 2012, 80(3):633-46
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.
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.
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).
S1179 WZ8040 WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I).
S2192 AZD8931 (Sapitinib) AZD8931 is a reversible, ATP competitive inhibitor of EGFR, ErbB2 and ErbB3 with IC50 of 4 nM, 3 nM and 4 nM, more potent than Gefitinib or Lapatinib against NSCLC cell, 100-fold more selective for the ErbB family than MNK1 and Flt. Phase 2.
  • Oncogene, 2014, 10.1038/onc.2014.161
  • J Immunol, 2014, 192(2):722-31
S1079 PD153035 HCl PD153035 is a potent and specific inhibitor of EGFR with Ki and IC50 of 5.2 pM and 29 pM; little effect noted against PGDFR, FGFR, CSF-1, InsR and Src.
  • J Immunol, 2012, 188(9):4581-9
  • Antivir Res, 2011, 89(1):64-70
  • Int J Clin Exp Pathol, 2014, 7(11):7663-7671
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).
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.
  • J Cell Biochem, 2014, 115(8):1381-91

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