Description
InformationASP5878 is a novelFGFR-selective inhibitor with IC50 values of 0.47, 0.60, 0.74, and 3.5 nmol/L for recombinant FGFR1, 2, 3, and 4, respectively.TargetsFGFR1 (Cell-free assay); FGFR2 (Cell-free assay); FGFR3 (Cell-free assay); FGFR4 (Cell-free assay) 0.47 nM; 0.6 nM; 0.74 nM; 3.5 nMIn vitroASP5878 inhibits the cell proliferation of HCC cell lines expressing FGF19. ASP5878 inhibits FGFR4 phosphorylation and its treatment results in the suppression of phosphorylation, mobility shift of FRS2, and suppression of ERK phosphorylation in Hep3B2.1-7 cells.In vivoOral administration of ASP5878 at 3 mg/kg induces sustained tumor regression in a subcutaneous xenograft mouse model using Hep3B2.1-7. In HuH-7, an orthotopic xenograft mouse model, ASP5878 induces complete tumor regression and dramatically extended the survival of the mice.Cell Research(from reference)Cell lines：Hep3B2.1-7 cells Concentrations：0-1000 nM Incubation Time：2 h