ASP-5878 (ASP5878) is a novel potent, selective pan-FGFR inhibitor with IC50 of 0.47/0.60/0.74/3.5 nM for FGFR1/2/3/4, respectively.
ASP-5878 also inhibits FGFR3 (K650E), FGFR3 (K650M), VEGFR2, FGFR4 (N535K), FMS with IC50 of 1.6, 4.2, 25, 78, 150 nM, respectively.
ASP-5878 potently suppressed the growth of the FGF19-expressing hepatocellular carcinoma cell lines Hep3B2.1-7, HuH-7, and JHH-7 with IC50 of 8.5-27 nM.
ASP-5878 induces sustained tumor regression in a xenograft mouse model using Hep3B2.1-7. Orally bioactive.
