E7090 succinate

E7090 (E 7090) is a potent, selective, orally available inhibitor of FGFR1, -2, and -3 with IC50 of 0.71, 0.50 and 1.2 nM, weakly inhibits FGFR4 (IC50=120 nM); inhibits only 3 tyrosine kinases (RET, DDR2, and FLT1) with IC50 lower than 10 nM among the 93 kinases, also potently inhibits mutant FGFR3 (K650E and K650M, IC50=3.1 and 16 nM); inhibits FGFR phosphorylation and cell proliferation of SNU-16 cells with IC50 of 1.2 and 5.7 nM, respectively; shows selective antiproliferative activity against cancer cell lines harboring FGFR abnormalities, exhibits antitumor activity and inhibits FGFR signaling in a mouse xenograft model of SNU-16 human gastric cancer. Solid Tumors Phase 1 Clinical

References 1. Watanabe Miyano S, et al. Mol Cancer Ther. 2016 Nov;15(11):2630-2639. View Related Products by Target FGFR Solid Tumors