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EGFR Inhibitors (37)

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.
  • 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, 2012, 483(7387):100-3
  • Nature, 2014, 508(7494):118-22
  • Cell, 2012, 151(5):937-50
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
  • Cancer Research, 2014, 74(1):341-52
  • Oncogene, 2013, 32(37):4427-35
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
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.
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 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.
  • Nat Commun, 2014, 5:3384
  • Proc Natl Acad Sci U S A, 2012, 109(17):6584-9
  • Oncogene, 2012, 32(37):4331-42
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
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, 2014, 35(4):795-806
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, 2014, 74(1):341-52
  • Cell Death Dis, 2014, 5:e1194
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
  • J Gastrointest Surg, 2013, 17(10):1723-31
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
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
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
  • Theriogenology, 2014, 81(4):572-8
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
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, 2011, 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
  • 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
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
Cat.No. Product Name Information Product Citations Customer Reviews
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
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).
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.
S1179 WZ8040 WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I).
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
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 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
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).
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.
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.
Cat.No. Product Name Information Product Citations Customer Reviews
S2406 Chrysophanic Acid Chrysophanic acid (Chrysophanol), a natural anthraquinone isolated from Dianella longifolia, is a EGFR/mTOR pathway inhibitor.
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).
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.
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.
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
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