Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Vecabrutinib (SNS-062) (SNS-062) 是一种有效的,非共价的 BTK 和 ITK 抑制剂,Kd 值分别为 0.3 nM 和 2.2 nM。Vecabrutinib 对 ITK 的 IC50 值为 24 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,310 | 现货 | ||
5 mg | ¥ 3,230 | 现货 | ||
10 mg | ¥ 4,730 | 现货 | ||
25 mg | ¥ 7,490 | 现货 | ||
50 mg | ¥ 9,870 | 现货 | ||
100 mg | ¥ 13,600 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 3,780 | 现货 |
产品描述 | Vecabrutinib (SNS-062) is a potent and noncovalent BTK and ITK inhibitor (Kd: 0.3 nM and 2.2 nM, respectively). Vecabrutinib displays an IC50 of 24 nM for ITK. |
靶点活性 | BTK:(kd)0.3 nM, ITK:2.2 nM(kd), ITK:24 nM |
体外活性 | Vecabrutinib is six times more potent than PCI-32765 and greater than 640 times more potent than acalabrutinib against C481S BTK. Vecabrutinib inhibits pBTK in human whole blood (average IC50: 50 nM). Vecabrutinib inhibits WT and C481S BTK with similar IC50s (pBTK IC50s: 2.9 nM and 4.4 nM for WT BTK and C481S BTK). In a recombinant kinase assay, IC50s of Vecabrutinib against WT BTK and C481S BTK are 4.6 nM and 1.1 nM. Vecabrutinib retains activity against the mutated BTK variant. Vecabrutinib demonstrates dose-dependent inhibition of BTK in primary patient CLL cells comparable to PCI-32765 via immunoblot for BTK phosphorylation. Vecabrutinib decreases the viability of primary CLL cells in the presence of HS5 stromal protection by 5.5% [1][2]. |
体内活性 | Vecabrutinib is well tolerated with continuous drug levels. Vecabrutinib has good oral bioavailability in rat and dog (%F ≥ 40%) and a terminal half-life of 5 to 6 hours [1]. |
别名 | SNS-062 |
分子量 | 529.92 |
分子式 | C22H24ClF4N7O2 |
CAS No. | 1510829-06-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 112.5 mg/mL (212.3 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.8871 mL | 9.4354 mL | 18.8708 mL | 47.1769 mL |
5 mM | 0.3774 mL | 1.8871 mL | 3.7742 mL | 9.4354 mL | |
10 mM | 0.1887 mL | 0.9435 mL | 1.8871 mL | 4.7177 mL | |
20 mM | 0.0944 mL | 0.4718 mL | 0.9435 mL | 2.3588 mL | |
50 mM | 0.0377 mL | 0.1887 mL | 0.3774 mL | 0.9435 mL | |
100 mM | 0.0189 mL | 0.0944 mL | 0.1887 mL | 0.4718 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。
Vecabrutinib 1510829-06-7 Angiogenesis Tyrosine Kinase/Adaptors Tyrosine Kinases BTK SNS 062 SNS-062 SNS062 Inhibitor inhibitor inhibit