BMS-986260 (E6646-GRP)

BMS-986260 is an orally active immuno-oncology agent that inhibits TGFβR1 with an IC50 of 1.6 nM. It shows selectivity for TGFβR1 compared to TGFβR2 and over 200 other kinases. In MINK and NHLF cell lines, BMS-986260 blocks TGFβ-induced pSMAD2/3 nuclear translocation with IC50 values of 350 nM and 190 nM, respectively.