产品描述:
CP 724,714 is a selective inhibitor of HER2/ErbB2 with an IC50 value of 10 nM.{31036} It demonstrates greater than 640-fold selectivity against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, and c-Met.{31036} CP 724,714 has been shown to inhibit the proliferation of ErbB2-amplified cells, including BT474 and SK-BR-3 with IC50 values of 0.25 and 0.95 μM, respectively.{31036} It also demonstrates antitumor activity in various human tumor xenograft models.{31036} However, CP 724,714 was discontinued from clinical development due to hepatotoxicity caused by its ability to inhibit hepatic efflux transporters at low micromolar concentrations.{31035}