EGFR

EGFR Inhibitors (40)

water-soluble

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 in cell-free assays, >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
  • Cancer Cell, 2015, 27(4):533-46
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
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-resistant L858R-T790M EGFR mutant.
  • Cancer Discov, 2013, 3(2):168-81
  • Gut, 2015, 10.1136/gutjnl-2014-309026
  • J Natl Cancer Inst, 2014, 106(9)
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
  • Cancer Lett, 2014, 344(1):90-100
  • J Cell Sci, 2010, 123(Pt 18):3102-11
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.
  • Cancer Cell, 2012, 21(4):488-503
  • Sci Transl Med, 2015, 7(284):284ra57
  • Gut, 2015, 10.1136/gutjnl-2014-309026
S7298 AZ5104 AZ5104, the demethylated metabolite of AZD-9291, is a potent EGFR inhibitor with IC50 of <1 nM, 6 nM, 1 nM, and 25 nM for EGFR (L858R/T790M), EGFR (L858R), EGFR (L861Q), and EGFR (wildtype), respectively. Phase 1.
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.
  • Cancer Discov, 2013, 3(2):168-81
  • Gut, 2015, 10.1136/gutjnl-2014-309026
  • J Natl Cancer Inst, 2014, 106(9)
S7557 CL-387785 (EKI-785) CL-387785 (EKI-785) is an irreversible, and selective EGFR inhibitor with IC50 of 370 pM.
  • Clin Cancer Res, 2015, 10.1158/1078-0432.CCR-14-2789
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.
  • Cell, 2012, 151(5):937-50
  • Nat Genet, 2012, 44(8):852-60
  • Cancer Cell, 2015, 27(4):533-46
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.
Cat.No. Product Name Information Product Use Citation Customer Product Validation
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.
  • Cancer Cell, 2012, 21(4):488-503
  • Sci Transl Med, 2015, 7(284):284ra57
  • Gut, 2015, 10.1136/gutjnl-2014-309026
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.
  • Cancer Discov, 2013, 3(2):168-81
  • Cancer Discov, 2013, 3(2):224-37
  • Cancer Discov, 2012, 2(5):458-71
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.
  • Clin Cancer Res, 2013, 19(17):4697-705
  • Cancer Lett, 2015, 359(2):335-43
  • Cancer Lett, 2013, 341(2):224-30
S1167 CP-724714 CP-724714 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 in cell-free assays. Phase 2.
  • Cancer Res, 2014, 74(1):341-52
  • Cell Death Dis, 2014, 5:e1194
  • Exp Cell Res, 2015, 332(2):223-35
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 EGFR T790M mutation. Phase 2.
  • Gut, 2015, 10.1136/gutjnl-2014-309026
  • J Immunol, 2013, 192(2):722-31
  • Cell Cycle, 2015, 14(4):648-55
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).
  • Nat Commun, 2015, 6:6377
  • Proc Natl Acad Sci USA, 2013, 110(38):E3595-604
  • Clin Cancer Res, 2015, 10.1158/1078-0432.CCR-15-0560
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 for the ErbB family than MNK1 and Flt. Phase 2.
  • Gut, 2015, 10.1136/gutjnl-2014-309026
  • Clin Cancer Res, 2015, 10.1158/1078-0432.CCR-14-2701
  • Oncogene, 2014, 10.1038/onc.2014.161
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
  • Bioorg Med Chem, 2015, 10.1016/j.bmc.2014.12.066
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.
  • Cell Rep, 2013, 4(4):764-75
  • J Pharmacol Exp Ther, 2012, 341(2):386-95
  • Toxicol Lett, 2014, 226(1):81-9
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.
  • Oncogene, 2015, 10.1038/onc.2015.59
  • J Immunol, 2012, 188(9):4581-9
  • Antivir Res, 2011, 89(1):64-70
Cat.No. Product Name Information Product Use Citation Customer Product Validation
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
  • J Cell Mol Med, 2013, 17(5):648-56
  • Head Neck, 2014, 10.1002/hed.23822.?
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
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).
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
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.
  • Clin Cancer Res, 2015, 10.1158/1078-0432.CCR-15-0560
  • J Thorac Oncol, 2015, 10.1097/JTO.0000000000000500
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
Cat.No. Product Name Information Product Use Citation Customer Product Validation
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).
  • Oncotarget, 2015, 5(12):4529-42
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.
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.
S2406 Chrysophanic Acid Chrysophanic acid (Chrysophanol), a natural anthraquinone isolated from Dianella longifolia, is a EGFR/mTOR pathway inhibitor.
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.
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.
  • Clin Cancer Res, 2015, 10.1158/1078-0432.CCR-15-0560
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All EGFR Products

Hover Mouse over '+' to display IC50

Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S1023 Erlotinib HCl (OSI-744) <1 mg/mL 3 mg/mL <1 mg/mL
S1025 Gefitinib (ZD1839) <1 mg/mL 89 mg/mL 4 mg/mL
S1011 Afatinib (BIBW2992) <1 mg/mL 97 mg/mL 15 mg/mL
S1019 Canertinib (CI-1033) <1 mg/mL 2 mg/mL 9 mg/mL
S2111 Lapatinib <1 mg/mL 100 mg/mL <1 mg/mL
S7298 AZ5104 <1 mg/mL 97 mg/mL 23 mg/mL
S7810 Afatinib (BIBW2992) Dimaleate <1 mg/mL 100 mg/mL <1 mg/mL
S7557 CL-387785 (EKI-785) <1 mg/mL 63 mg/mL <1 mg/mL
S7786 Erlotinib <1 mg/mL 78 mg/mL 21 mg/mL
S7358 Poziotinib (HM781-36B) <1 mg/mL 98 mg/mL <1 mg/mL
S1028 Lapatinib (GW-572016) Ditosylate <1 mg/mL 100 mg/mL <1 mg/mL
S2150 Neratinib (HKI-272) <1 mg/mL 2 mg/mL <1 mg/mL
S1143 AG-490 (Tyrphostin B42) <1 mg/mL 59 mg/mL 6 mg/mL
S1167 CP-724714 <1 mg/mL 94 mg/mL 94 mg/mL
S2727 Dacomitinib (PF299804, PF299) <1 mg/mL 19 mg/mL <1 mg/mL
S1173 WZ4002 <1 mg/mL 13 mg/mL <1 mg/mL
S2192 AZD8931 (Sapitinib) <1 mg/mL 40 mg/mL <1 mg/mL
S1194 CUDC-101 <1 mg/mL 20 mg/mL <1 mg/mL
S2728 AG-1478 (Tyrphostin AG-1478) <1 mg/mL 25 mg/mL 13 mg/mL
S1079 PD153035 HCl <1 mg/mL 0.5 mg/mL <1 mg/mL
S1392 Pelitinib (EKB-569) <1 mg/mL 13 mg/mL <1 mg/mL
S1056 AC480 (BMS-599626) <1 mg/mL 113 mg/mL 20 mg/mL
S1486 AEE788 (NVP-AEE788) <1 mg/mL 88 mg/mL <1 mg/mL
S2205 OSI-420 <1 mg/mL 83 mg/mL <1 mg/mL
S1170 WZ3146 <1 mg/mL 93 mg/mL <1 mg/mL
S1179 WZ8040 <1 mg/mL 96 mg/mL 3 mg/mL
S2185 AST-1306 <1 mg/mL 124 mg/mL <1 mg/mL
S7284 Rociletinib (CO-1686, AVL-301) <1 mg/mL 100 mg/mL <1 mg/mL
S1342 Genistein <1 mg/mL 54 mg/mL 2 mg/mL
S2755 Varlitinib <1 mg/mL 6 mg/mL <1 mg/mL
S2922 Icotinib <1 mg/mL 78 mg/mL 7 mg/mL
S2784 TAK-285 <1 mg/mL 110 mg/mL 54 mg/mL
S2867 WHI-P154 <1 mg/mL 75 mg/mL <1 mg/mL
S7039 PD168393 <1 mg/mL 74 mg/mL <1 mg/mL
S7206 CNX-2006 <1 mg/mL 100 mg/mL 29 mg/mL
S2895 Tyrphostin 9 <1 mg/mL 56 mg/mL 56 mg/mL
S8009 AG-18 <1 mg/mL 37 mg/mL 37 mg/mL
S2406 Chrysophanic Acid <1 mg/mL 5 mg/mL <1 mg/mL
S8036 Butein <1 mg/mL 55 mg/mL 55 mg/mL
S7297 AZD9291 <1 mg/mL 99 mg/mL 43 mg/mL
Tags: EGFR inhibition | EGFR cancer | EGFR tumor | EGFR activation | EGFR signaling pathway | EGFR phosphorylation | EGFR targets | EGFR inhibitor drugs | EGFR inhibitors cancer | EGFR assay | EGFR activity | EGFR inhibitors list | EGFR inhibitor review
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