Vecabrutinib
作者：齐岳
发布时间：2023-08-23
09:17:16
点击数：
产品名称：Vecabrutinib
产品描述：
| 产品描述 | Vecabrutinib 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 | Itk:2.2 nM（kd）, Itk:24 nM, BTK:（kd）0.3 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 |
存储
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 112.5mg/mL (212.3mM),Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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