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首页-小分子抑制剂&激动剂-Tyrosine Kinase-BTK-Vecabrutinib
Vecabrutinib

Chemical Structure : Vecabrutinib

CAS No.: 1510829-06-7

Vecabrutinib (SNS 062, SNS062, SNS-062)

货号: PC-50001Not For Human Use, Lab Use Only.

Vecabrutinib (SNS-062) is a potent, reversible, non-covalent BTK inhibitor with IC50 of 2.9 and 4.4 nM for WT BTK and C481S BTK, respectively.

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生物&药学活性

Vecabrutinib (SNS-062) is a potent, reversible, non-covalent BTK inhibitor with IC50 of 2.9 and 4.4 nM for WT BTK and C481S BTK, respectively.
Vecabrutinib (SNS-062) binds to Tec kinase family members BTK (Kd=0.3 nM) and ITK (Kd=2.2 nM), but not bind EGFR, active in vitro in cells with the C481S mutation.
Vecabrutinib (SNS-062) inhibits pBTK in human whole blood with IC50 of 50 nM, demonstrates favorable pharmacokinetic properties.
Vecabrutinib (SNS-062) shows potential for overcoming the ibrutinib resistance due to C481S mutantion in BTK.

物理化学性质&存储条件

分子量 529.925
分子式 C22H24ClF4N7O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping Room temperature in continental US; may vary elsewhere
Solubility

10 mM in DMSO

Chemical Name/SMILES

(3R,3'R,4'S)-1'-(6-amino-5-fluoropyrimidin-4-yl)-3-[3-chloro-5-(trifluoromethyl)anilino]-2-oxo[1,3'-bipiperidine]-4'-carboxamide

参考文献

1. Thompson PA, et al. Expert Opin Investig Drugs. 2017 Nov 15:1-12.

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