化合物 T14357 T14357

Product Introduction
Bioactivity


英文名: Spebrutinib besylate

描述: Spebrutinib besylate (AVL-292 benzenesulfonate; CC-292 besylate) is a Btk kinase activity inhibitor (IC50<0.5 nM, Kinact/Ki=7.69×104 M-1s-1s).

体外活性: 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. Spebrutinib (CC-292) is a covalent, highly selective, orally active inhibitor of Btk with IC50 value of 0.5 nM. 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]. 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).

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: benzenesulfonate | AVL 292 | AVL292 | CC 292 | CC292 | besylate | CC-292 | Spebrutinib besylate | AVL-292

相关产品: BTK-IN-16 | BTK-IN-25 | N-piperidine Ibrutinib hydrochloride | CHMFL-BTK-01 | ARQ 531 | Sunvozertinib | (R)-Zanubrutinib | JNJ-64264681 | Remibrutinib | IBT6A

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途