Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Description
BMS-986142 is a potent and highly selective reversible small molecule inhibitor of BTK with an IC50 of 0.5 nM. In a panel of 384 kinases, only five kinases were inhibited by BMS-986142 with less than 100-fold selectivity for BTK (TEC, ITK, BLK, TXK and BMX).
In B cells stimulated through the B cell receptor (BCR), BMS-986142 potently inhibits signaling and functional end points, including calcium flux (IC50 = 9 nM), production of cytokines, proliferation, and surface expression of the costimulatory molecule CD86 (IC50 = 3−4 nM). In T cells, ITK-catalyzed phosphorylation of PLCγ1 stimulated through the T cell receptor (TCR) is at least 45-fold less potently inhibited by BMS-986142 than BTK-dependent signaling end points in B cells, as expected based on the 30-fold selectivity for BTK over ITK in the enzymatic assays.