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ErbB4 Inhibitors

  • EGFR/ErbB1
  • HER2/ErbB2
  • ErbB3
  • ErbB4
Kat.-Nr. Produktname Informationen Selektiv / Pan IC50 / Ki
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 ErbB4, IC50: 0.8 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 HER4, IC50: 23.5 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 ErbB4, IC50: 73.7 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 HER4/ErbB4, IC50: 160 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 HER4, IC50: 190 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 HER4, IC50: 260 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 ErbB4, IC50: 367 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 ErbB4, IC50: 367 nM