Spebrutinib besylate,1360053-8

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Spebrutinib besylate

CAS No. : 1360053-81-1

MCE 国际站：Spebrutinib besylate

产品活性：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。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：Btk

In Vitro: Spebrutinib (CC-292) is a covalent, highly selective, orally active inhibitor of Btk with IC₅₀ value 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 EC₅₀ of Btk occupancy from a Spebrutinib dose-response in Ramos cells (EC₅₀=6 nM) correlated directly with the cellular EC₅₀ of 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.

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