– BMS-986260 is a potent, selective, and orally bioavailable TGF?R1 inhibitor (IC50=1.6 nM). BMS-986260 demonstrated functional activity in multiple TGF?-dependent cellular assays, excellent kinome selectivity, favorable pharmacokinetic properties, and curative in vivo efficacy in combination with anti-PD-1 antibody in murine colorectal cancer (CRC) models.