BMS-935177 is a potent and selective, orally bioavailable, reversible BTK inhibitor with IC50 of 2.8 nM.
BMS-935177 displays 5-67-fold selectivity over Tec family kinases, 7-fold selectivity over BLK, and 56-fold over Lck in panel of 384 kinases.
BMS-935177 effectively inhibits TNFα production in PBMCs (IC50=14 nM), inhibits CD69 surface expression in human and mouse whole blood (IC50=0.55 and 2.06 uM, respectively).
BMS-935177 shows profound efficacy in the CAIA and CIA models of arthritis.
