HDAC-IN-50, a potent, orally active inhibitor targeting both FGFR (Fibroblast Growth Factor Receptor) and HDAC (Histone Deacetylase), exhibits IC50 values of 0.18, 1.2, 0.46, 1.4, 1.3, 1.6, 2.6, 13 nM for FGFR1, FGFR2, FGFR3, FGFR4, HDAC1, HDAC2, HDAC6, HDAC8, respectively. This dual inhibitor induces apoptosis and cell cycle arrest at the G0/G1 phase while decreasing the expression of phosphorylated FGFR1 (pFGFR1), phosphorylated ERK (pERK), and phosphorylated STAT3 (pSTAT3), thus demonstrating anti-tumor activity.

FGFR3:0.46 nM, HDAC8:13 nM, FGFR1:0.18 nM, HDAC6:2.6 nM, HDAC1:1.3 nM, FGFR4:1.4 nM, HDAC2:1.6 nM, FGFR2:1.2 nM