Branebrutinib (BMS-986195)
分子式：C20H23FN4O2分子量： 370.42
简介：Branebrutinib (BMS-986195)是有效的BTK抑制剂，对BTK, TEC, BMX, TXK的IC50值分别为0.1 nM, 0.9 nM, 1.5 nM, 5 nM。
物理性状及指标：
外观：……………………粉末
溶解性：…………………DMSO: 74 mg/mL (199.77 mM)；Ethanol：38 mg/mL (102.59 mM)；Water：Insoluble
含量：……………………>98%
储存温度：-20℃，避光防潮密闭干燥
生物活性
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描述 |
Branebrutinib (BMS-986195)是有效的BTK抑制剂，对BTK, TEC, BMX, TXK的IC50值分别为0.1 nM, 0.9 nM, 1.5 nM, 5 nM。 | ||||||||
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靶点 |
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体外 |
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). | ||||||||
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体内 |
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 (<5% of plasma concentration). Both the plasma T1/2(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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动物实验 |
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储液配置及储存：按表中溶解性配置；如溶解困难，可以通过快速搅拌，超声或温和加热（在45-60°C下水浴）。液体稳定性报道的很少，建议现配现用，如需储存，建议：-20℃1-3月；-80℃ 3-6月。
| 浓度/体积/质量 |
1 mg |
5 mg |
10 mg |
| 1 mM | 2.6996 mL | 13.4982 mL | 26.9964 mL |
| 5 mM | 0.5399 mL | 2.6996 mL | 5.3993 mL |
| 10 mM | 0.2700 mL | 1.3498 mL | 2.6996 mL |
| 50 mM | 0.0540 mL | 0.2700 mL | 0.5399 mL |
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