BMS 986142

BTK抑制剂(IC50=0.5nM)；在384种激酶中，对BTK的选择性超过20倍；抑制BCR刺激诱导的RamosB细胞钙通量(IC50=9nM)，以及BCR刺激诱导的外周B细胞增殖和CD86表面表达(IC50分别为3和4nM)；抑制Fcγ受体刺激诱导的人类PBMCs中的TNF-α产生(IC50=3nM)；每天30mg/kg剂量可降低NZB/W狼疮易感小鼠模型中严重蛋白尿小鼠的百分比并提高生存率；5和20mg/kg剂量可减少CAIA小鼠模型中后爪胫跗关节骨吸收和炎症。A BTK inhibitor (IC50 = 0.5 nM); greater than 20-fold selective for BTK over a panel of 384 kinases; inhibits BCR stimulation-induced calcium flux in Ramos B cells (IC50 = 9 nM), as well as BCR stimulation-induced proliferation of, and CD86 surface expression in, peripheral B cells (IC50s = 3 and 4 nM, respectively); inhibits by Fcγ receptor stimulation-induced TNF-α production in human PBMCs (IC50 = 3 nM); reduces the percentage of mice with severe proteinuria and increases survival in an NZB/W lupus-prone mouse model at 30 mg/kg per day; reduces hind paw tibiotarsal joint bone resrption and inflammation in a CAIA mouse model at 5 and 20 mg/kg.分子式C32H30F2N4O4分子量572.6CC(C)(O)C(C1)CCC2=C1NC3=C2C(C4=CC=CC(N5C(N(C)C(C(F)=CC=C6)=C6C5=O)=O)=C4C)=C(F)C=C3C(N)=O