BMS 986260

An ALK5 inhibitor (IC50 = 0.0015 µM); selective for ALK over TGF-βRII (IC50 = > 15 µM) and a panel of 213 additional kinases at 1 µM; inhibits TGF-β-induced increases in the nuclear translocation of phosphorylated SMAD2/3 in Mv 1 Lu cells (IC50 = 0.35 µM); decreases tumor growth in an MC-38 murine colon carcinoma model of tumor rechallenge at 3.75 mg/kg per day in combination with an antibody against PD-1; induces hyperproliferation of chondrocytes in the femoral epiphysis, thickening of the cardiac atrioventricular valve, and inflammation in the aortic vasculature in rats at 10 mg/kg per day