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Spebrutinib besylate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Spebrutinib besylate图片
CAS NO:1360053-81-1
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
AVL-292 benzenesulfonate
CC-292 besylate
产品介绍
Spebrutinib besylate (AVL-292 benzenesulfonate; CC-292 besylate) 是共价,高选择性和口服活性的Btk抑制剂,IC50为0.5 nM。
生物活性

Spebrutinib besylate (AVL-292 benzenesulfonate; CC-292 besylate) is a potent inhibitor ofBtkkinase activity (IC50<0.5 nM,Kinact/Ki=7.69×104M-1s-1s) in biochemical assays.

IC50& Target

IC50:<0.5 nM (Btk)[1]

体外研究
(In Vitro)

Spebrutinib (CC-292) is a covalent, highly selective, orally active inhibitor of Btk with IC50value of 0.5 nM. Spebrutinib also less potently inhibits Yes, c-Src, Brk, Lyn, and Fyn with IC50s of 723 nM, 1.729 μM, 2.43 μM, 4.4 μM, and 7.15 μM, rspectively. Extensive analysis has revealed that the EC50of Btk occupancy from a Spebrutinib dose-response in Ramos cells (EC50=6 nM) correlated directly with the cellular EC50of Btk kinase inhibition with Spebrutinib (EC50=8 nM). Furthermore, the concentration at which Spebrutinib inhibits 90% of Btk activity in Ramos cells is 35 nM while the concentration of Spebrutinib required for 90% occupancy of Btk is 39 nM[1].

Clinical Trial
分子量

581.62

Formula

C28H28FN5O6S

CAS 号

1360053-81-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.