产品描述:
BGJ398 is an orally available inhibitor of human FGFRs (IC50s = 0.9, 1.4, and 1 nM for FGFR1, FGFR2, and FGFR3, respectively).{31102,30600} It inhibits FGFR4 and VEGFR2 with IC50 values of 60 and 180 nM, respectively, and displays comparatively little activity towards Abl, Fyn, Kit, Lck, Lyn, and Yes (IC50s = 0.3-2.5 µM).{31102} BGJ398 has been shown to suppress the proliferation of cancer cells with wild-type FGFR3 overexpression (IC50s = 5, 30, 32, and 15 nM, for RT112, RT4, SW780, and JMSU1 cells, respectively).{31102} In an RT112 bladder cancer xenograft mouse model overexpressing wild-type FGFR3, BGJ398 inhibited tumor growth after oral administration of 10-30 mg/kg.{31102}