BMS-935177 is a reversible BTK inhibitor with IC50 value of 3 nM.

BTK:3 nM

In human Ramos B cells, BMS-935177 inhibits calcium flux with an IC50 of 27 nM. BMS-935177 inhibits CD69 surface expression in peripheral B cells stimulated with antiIgM and anti-IgG. Against IgG-containing immune complexdriven low affinity activating FcγRIIa and FcγRIII end points in peripheral blood mononuclear cells, BMS-935177 effectively inhibits TNFα production (IC50 = 14 nM). BMS-935177 shows mean IC50 values of 550 and 2060 nM in human and mouse whole blood, respectively[1].

BMS-935177(5, 20, and 45 mg/kg) inhibits anti-KLH antibodies of the IgG isotype at day 14, with statistically significant reductions at all doses. In satellite mice, BMS-935177 (5 mg/kg) maintains the plasma concentration above the mouse whole blood BCR-stimulated CD69 IC50 value of 2 μM for only 5 h. BMS-935177(10, 20, and 30 mg/kg) provides dose-dependently reduces both the severity and incidence of clinically evident disease in this rodent model of RA. BMS-935177(10 mg/kg) reduces the disease severity about 40%, and the percentage of animals showing any signs of disease is reduced by a third[1].