Information Branebrutinib (BMS-986195) Branebrutinib (BMS-986195) is a potent inhibitor of BTK with IC50 values of 0.1 nM, 0.9 nM, 1.5 nM, 5 nM for BTK, TEC, BMX, TXK, respectively. Targets BTK (Cell-free assay); TEC (Cell-free assay); BMX (Cell-free assay); TXK (Cell-free assay) 0.1 nM; 0.9 nM ;1.5 nM; 5 nM In vitro In human whole blood assays, BMS-986195 potently inhibited BCR-stimulated expression of CD69 on B cells with an IC50 of 11 nM. BMS-986195 is highly selective, providing >5,000-fold selectivity for BTK over 240 kinases with only the 4 related Tec family kinases demonstrating less than 5000-fold selectivity (9 - 1,000-fold). In vivo In multi-species pharmacokinetic studies, the absolute oral bioavailability of BMS-986195 is 100% in mice, 74% in rats, 46% in cynomolgus monkeys, and 81% in dogs. The total body plasma clearance of BMS-986195 is low in all species. The steadystate volume of distribution observed is greater than the plasma volume but less than the total body water, indicative of extravascular distribution, in spite of the high protein binding (free fraction: 0.2-1.2%). Brain penetration is very low in mice, rats, and dogs ( 1/2 (i.v.) and Tmax (p.o.) values were short across species (0.46-4.3 h and 0.58-1.0 h, respectively）.
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Branebrutinib (BMS-986195)
CAS number：1912445-55-6 molecular formula：C20H23FN4O2
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| Chinese alias | (S)-4-(3-(丁-2-炔基)哌啶-1-基)-5-氟-2,3-二甲基-1H-吲哚-7-甲酰胺 | ||
| English alias | 4-((3S)-3-(2-Butynoylamino)-1-piperidinyl)-5-fluoro-2,3-dimethyl-1H-indole-7-carboxamide | 4-((3S)-3-(2-BUTYNOYLAMINO)-1-PIPERIDINYL)-5-FLUORO-2,3-DIMETHYL-1HINDOLE-7-CARBOXAMIDE | (S)-4-(3-(2-BUTYNOYLAMINO)PIPERIDIN-1-YL)-5-FLUORO-2,3-DIMETHYL-1H-INDOLE- | ||
| CAS number | 1912445-55-6 | molecular formula | C20H23FN4O2 |
| molecular weight | 370.42 g/mol | Exact mass | - |
| PSA | 91.200 Ų | logp | 2.8 |
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