BMS-986260, an immuno-oncology agent, is a potent, selective, and orally activeTGFβR1inhibitor (IC₅₀=1.6 nM). BMS-986260 displays exquisite selectivity for TGFβR1 over its isozyme TGFβR2, as well as in a panel of more than 200 kinases examined. BMS-986260 inhibits TGFβ mediated nuclear translocation of pSMAD2/3 in MINK and NHLF cells lines with an IC₅₀of 350 nM and 190 nM, respectively^[1].

BMS-986260 is a highly potent TGFβR1 inhibitor in both human (K_iapp=0.8 nM) and mouse (K_iapp= 1.4 nM) biochemical assays. BMS-986260 also inhibits TGFβ induced SMAD phosphorylation in NIH3T3 cell line, primary human T cells, and mouse and human whole blood. BMS-986260 inhibits TGF-β mediated induction of regulatory T cell (Treg) by downregulation of FOXP3 expression and a repression of CD25 with an IC₅₀of 230 nM^[1].

382.78

Solid

C₁₈H₁₂ClFN₆O

2001559-19-7

Room temperature in continental US; may vary elsewhere.