布仑布替尼（BMS-986195）
规格
| Cas Number | 1912445-55-6 |
| 规格或纯度 | Moligand™, ≥99% |
| 级别 | Moligand™ |
| 纯度 | ≥99% |
| 包装 | 100mg 或 50mg 或 10mg 或 5mg 或 25mg 或 2mg |
产品信息
| 别名 | (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 |
| 品牌 | 阿拉丁 |
| Action Type | 抑制剂 |
| Mechanism Of Action | 布鲁顿酪氨酸激酶抑制剂 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 74 mg/mL (199.77 mM); Ethanol: 38 mg/mL (102.58 mM); Water: Insoluble; |
| 简短描述 | BTK抑制剂 |
| 英文简短描述 | BTK Inhibitors |
| 过滤标签 | Bruton tyrosine kinase Inhibitor,Btk,Protein Tyrosine Kinase/RTK |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | 布莱恩布替尼（BMS-986195）是一种强效的 BTK 抑制剂，对 BTK、TEC、BMX 和 TXK 的 IC50 值分别为 0.1 nM、0.9 nM、1.5 nM 和 5 nM。 |
| 英文描述 |
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 (<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）. |