Information BMS-935177 is a potent, reversibleBruton's Tyrosine Kinase (BTK)inhibitor with an IC50 value of 2.8 nM and demonstrates good kinase selectivity. It is more potent against BTK than other kinase, including the other Tec family kinases (TEC, BMX, ITK, and TXK) over which the compound is between 5- and 67-fold selective. Targets BTK (Cell-free assay); TEC (Cell-free assay); BLK (Cell-free assay); BMX (Cell-free assay); TrkA (Cell-free assay) 29234,2.8 nM; 13 nM; 20 nM; 24 nM; 30 nM In vitro BMS-935177 shows greater than 50-fold selectivity over the SRC family of kinases, including 1100-fold selectivity over SRC itself. Other kinases inhibited with a potency less than 150 nM (50-fold selectivity) included TRKA, HER4, TRKB, and RET. It inhibits calcium flux in human Ramos B cells (IC50 = 27 nM) and inhibits CD69 surface expression in peripheral B cells stimulated with anti-IgM 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 complex-driven low affinity activating Fcγ receptor (FcγRIIa and FcγRIII) end points in peripheral blood mononuclear cells (PBMCs), BMS-935177 effectively inhibited TNFα production with an IC50 value of 14 nM. In vivo Plasma protein binding for BMS-935177 is high for all species, with less than 1% free for human. It has excellent oral bioavailability in all preclinical species, from both suspension and solution dosing, despite its low aqueous solubility. The oral bioavailability for BMS-935177 with solution dosing ranges from 84% to 100% in rat, mouse, dog, and cynomolgus monkey, with low clearance in single intravenous (iv) infusion studies. When dosed at 2 mg/kg i.v. in mouse and rat, the T 1/2 of BMS-935177 is 4 h and 5.1 h respectively.
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BMS-935177
CAS number：1231889-53-4 molecular formula：C31H26N4O3
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| Chinese alias | - | ||
| English alias | 9H-Carbazole-1-carboxamide,7-(1-hydroxy-1-methylethyl)-4-[2-methyl-3-(4-oxo-3(4H)-quinazolinyl)phenyl]- | ||
| CAS number | 1231889-53-4 | molecular formula | C31H26N4O3 |
| molecular weight | 502.56 g/mol | Exact mass | 10mM in DMSO |
| PSA | 112.000 Ų | logp | 4.500 |
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