BMS-935177,1231889-53-4

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BMS-935177

CAS No. : 1231889-53-4

MCE 国际站：BMS-935177

产品活性：BMS-935177是有效，选择性，可逆的布鲁顿酪氨酸激酶 (Btk) 抑制剂，IC₅₀ 值为3 nM。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：Btk

In Vitro: In B cells stimulated through the BCR, BMS-935177 selectively inhibits several different readouts. BMS-935177 inhibits calcium flux in human Ramos B cells (IC₅₀=27 nM) and inhibits CD69 surface expression in peripheral B cells stimulated with antiIgM and anti-IgG. However, BMS-935177 has no effect on CD69 surface expression in B cells stimulated through the CD40 receptor with CD40 ligand. Against IgG-containing immune complexdriven low affinity activating Fcγ receptor (FcγRIIa and FcγRIII) end points in peripheral blood mononuclear cells (PBMCs), BMS-935177 effectively inhibits TNFα production with an IC₅₀ value of 14 nM. BMS-935177 shows mean IC₅₀ values of 550±100 (n=11) and 2060±240 nM (n=3) in human and mouse whole blood, respectively.

In Vivo: When dosed orally once daily at 5, 20, and 45 mg/kg to mice, BMS-935177 inhibits anti-KLH antibodies of the IgG isotype at day 14, with statistically significant reductions at all doses. In satellite mice from this study dosed with 6 at 5 mg/kg, the plasma concentration is maintained above the mouse whole blood BCR-stimulated CD69 IC₅₀ value of 2 μM for only approximately 5 h. At once daily oral doses of 10, 20, and 30 mg/kg beginning on the day of primary immunization, BMS-935177 provides a clear dose-dependent reduction in both the severity and incidence of clinically evident disease in this rodent model of RA. At 10 mg/kg of BMS-935177, disease severity is reduced about 40% compared to vehicle treatment, and the percentage of animals showing any signs of disease is reduced by a third.

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