Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Branebrutinib (BMS986195) 是一个高效的、不可逆的、共价的、选择抑的布鲁顿氏酪氨酸激酶(BTK)的制剂 (IC50:0.1 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 453 | 现货 | ||
2 mg | ¥ 659 | 现货 | ||
5 mg | ¥ 1,330 | 现货 | ||
10 mg | ¥ 1,990 | 现货 | ||
25 mg | ¥ 3,370 | 现货 | ||
50 mg | ¥ 4,790 | 现货 | ||
100 mg | ¥ 6,690 | 现货 | ||
200 mg | ¥ 8,830 | 现货 | ||
500 mg | ¥ 13,300 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,260 | 现货 |
产品描述 | Branebrutinib (BMS986195) is a potent, covalent inhibitor of Bruton's tyrosine kinase (BTK), >5,000-fold selective over all kinases outside of the Tec family (IC50 <1 nM for BTK). |
靶点活性 | BTK:<1 nM (cell free) |
体外活性 | BMS-986195 inactivated BTK in human whole blood with a rapid rate of inactivation (3.5×10^-4 /nM/min) and potently inhibited antigen-dependent interleukin-6 production, CD86 expression and proliferation in B cells (IC50 <1 nM) without effect on antigen-independent measures in the same cells. A similar potency was measured against FcγR-dependent TNF-α production in human cells. |
体内活性 | In mice, a dose as low as 0.5 mg/kg, taken orally (PO) daily (QD), resulted in peak BTK inactivation of 98% after only the second dose. BTK was inactivated to similar levels in whole blood, lymph nodes and spleen in a dose-dependent manner. BMS-986195 demonstrated robust efficacy in murine models of RA including CIA and CAIA, protecting against clinically evident disease, histologic joint damage and bone mineral density loss. In both models, maximal efficacy was observed at doses ≤0.5 mg/kg PO QD, which achieved ≥95% inactivation of BTK in vivo. |
别名 | BMS986195 |
分子量 | 370.42 |
分子式 | C20H23FN4O2 |
CAS No. | 1912445-55-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (269.96 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6996 mL | 13.4982 mL | 26.9964 mL | 67.491 mL |
5 mM | 0.5399 mL | 2.6996 mL | 5.3993 mL | 13.4982 mL | |
10 mM | 0.27 mL | 1.3498 mL | 2.6996 mL | 6.7491 mL | |
20 mM | 0.135 mL | 0.6749 mL | 1.3498 mL | 3.3745 mL | |
50 mM | 0.054 mL | 0.27 mL | 0.5399 mL | 1.3498 mL | |
100 mM | 0.027 mL | 0.135 mL | 0.27 mL | 0.6749 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Branebrutinib 1912445-55-6 Angiogenesis Tyrosine Kinase/Adaptors BTK Inhibitor Btk BMS986195 BMS 986195 inhibit Bruton tyrosine kinase BMS-986195 inhibitor