In Vitro: ASP5878 shows potent antiproliferative activity in most human HCC cell lines. ?ASP5878 inhibits FGFR4 phosphorylation in a concentration-dependent manner. ASP5878 treatment results in the suppression of phosphorylation, mobility shift of FRS2, and suppression of ERK phosphorylation.
In Vivo: ASP5878 (3 mg/kg, orally, once daily) shows antitumor activity in a Hep3B2.1-7 subcutaneous xenograft? and HCC orthotopic xenograft mouse model. ?ASP5878 induces shrinkage of FGF19-expressing HCC xenograft model.