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Vecabrutinib (Synonyms: SNS-062) 纯度: 99.85%
Vecabrutinib (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。
Vecabrutinib Chemical Structure
CAS No. : 1510829-06-7
规格 | 价格 | 是否有货 | 数量 |
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10 mM * 1 mL in DMSO | ¥4660 | In-stock | |
5 mg | ¥4000 | In-stock | |
10 mg | ¥6500 | In-stock | |
25 mg | ¥13500 | In-stock | |
50 mg | ¥22000 | In-stock | |
100 mg | ¥34000 | In-stock | |
200 mg | 询价 | ||
500 mg | 询价 |
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Vecabrutinib 相关产品
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生物活性 |
Vecabrutinib (SNS-062) is a potent, noncovalent BTK and ITK inhibitor, with Kd values of 0.3 nM and 2.2 nM, respectively. Vecabrutinib shows an IC50 of 24 nM for ITK[1][2]. |
IC50 & Target |
IC50: 24 nM (ITK)[2] |
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体外研究 (In Vitro) |
Vecabrutinib inhibits pBTK in human whole blood with an average IC50 of 50 nM. Vecabrutinib inhibits WT and C481S BTK with similar IC50s (pBTK IC50s: WT BTK 2.9 nM, C481S BTK 4.4 nM)[1]. 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 is six times more potent than PCI-32765 and greater than 640 times more potent than acalabrutinib against C481S BTK. Vecabrutinib demonstrates dose-dependent inhibition of BTK in primary patient CLL cells comparable to PCI-32765 via immunoblot for BTK phosphorylation. Vecabrutinib decreases viability of primary CLL cells in the presence of HS5 stromal protection by 5.5%[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
Vecabrutinib has good oral bioavailability in rat and dog (%F ≥ 40%) and a terminal half-life of 5 to 6 hours. Vecabrutinib is well tolerated with continuous drug levels and at exposures much greater than those achieved for PCI-32765[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Clinical Trial |
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分子量 |
529.92 |
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Formula |
C22H24ClF4N7O2 |
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CAS 号 |
1510829-06-7 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : 125 mg/mL (235.88 mM; Need ultrasonic) 配制储备液
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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