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EGFR Inhibitors (34)

water-soluble

Cat.No. Product Name Information Product Citations Customer Reviews
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. Phase 3.
  • Nat Genet, 2012, 44(8):852-60
  • Cell, 2012, 151(5):937-50
  • 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, 2012, 483(7387):100-3
  • Cell, 2012, 151(5):937-50
  • Mol Syst Biol, 2011, 7:486
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. Phase 3.
  • Cancer Discov, 2013, 3(2):168-81
  • Clin Cancer Res, 2012, 18(6):1663-71
  • Oncogene, 2013, 32(37):4427-35
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
  • Mol Oncol, 2012, 7(3):392-401
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
  • Clin Cancer Res, 2012, 18(6):1663-71
  • Oncogene, 2013, 32(37):4427-35
S8009 AG-18 AG-18 inhibits EGFR with IC50 of 35 μM.
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.
S7284 CO-1686 (AVL-301) CO-1686 is an irreversible, mutant-selective EGFR inhibitor with Ki of 21.5 nM and 303.3 nM for EGFRL858R/T790M and EGFRWT, respectively. Phase 1/2.
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.
  • Proc Natl Acad Sci U S A, 2012, 109(17):6584-9
  • Oncogene, 2012, 32(37):4331-42
  • Carcinogenesis, 2010, 31(11):1948-55
Cat.No. Product Name Information Product Citations Customer Reviews
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, 2012, 2(5):458-71
  • Cancer Discov, 2013, 3(2):168-81
  • Cancer Discov, 2013, 3(2):224-37
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 Gastrointest Surg, 2013, 17(10):1723-31
  • J Immunol, 2013, 192(2):722-31
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
  • Prostate, 2012, 73(3):267-77
  • Biochem Biophys Res Commun, 2013, 429(3-4):156-62
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.
  • ACS Medicinal Chemistry Letters, 2013, Qingqing Meng
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 1/2.
  • J Immunol, 2013, 192(2):722-31
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.
  • PLoS ONE, 2013, 8(8): e70353
  • Toxicol Lett, 2014, 10.1016/j.toxlet.2014.01.035
  • Cell Rep, 2013, 4(4):764-75
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.
  • Antivir Res, 2010, 89(1):64-70
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
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
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
Cat.No. Product Name Information Product Citations Customer Reviews
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, 2013, 74(1):341-52
S1486 AEE788 (NVP-AEE788) 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.
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.
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). Phase 4.
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
  • Cancer Res, 2012, 72(12):3069-79
  • J Cell Mol Med, 2013, 17(5):648-56
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.
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,
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.
S2755 Varlitinib ARRY334543 is a selective and potent ErbB1(EGFR) and ErbB2(HER2) inhibitor with IC50 of 7 nM and 2 nM, respectively. Phase 2.
  • Journal of Cellular Biochemistry, 2014, 10.1002/jcb.24787
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.
Cat.No. Product Name Information Product Citations Customer Reviews
S2826 Desmethyl Erlotinib (CP-473420, OSI-774) Desmethyl Erlotinib (CP-473420, OSI-774) is a free base of OSI-420, the active metabolite of Erlotinib (EGFR inhibitor with IC50 of 2 nM).
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).
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