Poseltinib 是一种具有口服活性，选择性，不可逆的小分子Bruton酪氨酸激酶 (BTK) 抑制剂，IC50 为 1.95 nM，对 BMX，TEC 和 TXK 的选择性作用分别是 0.3，2.3 和 2.4 倍。Poseltinib可共价结合 BTK 的活性位点 (半胱氨酸 481 残基)，同时有效抑制 B 细胞受体 (BCR)，Fc受体 (FcR)，Toll样受体 (TLR) 介导的信号传导。
货号:ajcx29606
CAS:1353552-97-2
分子式:C26H26N6O3
分子量：470.52
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Poseltinib, an orally active, selective and irreversible Bruton's tyrosine kinase (BTK) inhibitor (IC50 =1.95 nM), with 0.3, 2.3 and 2.4-fold selectivity for BTK over BMX, TEC and TXK, respectively. Poseltinib can covalently bind to the active site (cysteine 481 residue) of BTK, and reveales potent inhibition of B cell receptor (BCR), Fc receptor (FcR), Toll-like receptor (TLR) mediated signaling[1].

[1]. Kim YY, et al. HM71224, a selective Bruton's tyrosine kinase inhibitor, attenuates the development of murine lupus. Arthritis Res Ther. 2017 Sep 26;19(1):211.