CAS:1353552-97-2Poseltinib

Synonyms: HM71224;LY-3337641

Poseltinib is a tyrosine kinase inhibitor of Bruton's tyrosine kinase (BTK).

规格	价格	促销价格	库存

18817579266

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咨询

18817579266

立即询价

实验数据

技术信息

CAS号

1353552-97-2

储存条件

分子式

C26H26N6O3

运输

蓝冰

分子量

470.52

别名

HM71224;LY-3337641

溶解度

DMSO	77.5 mg/mL (164.7 mM)
Water	insoluble

动物实验配方

生物活性

描述Bruton's tyrosine kinase (BTK), a member of the Tec family of tyrosine kinases and expressed in B cells, macrophages, and monocytes but not in T cells, plays a crucial role in signaling through the B cell receptor (BCR) and the Fcγ receptor (FcγR) in B cells and myeloid cells, respectively. Poseltinib, an orally active, selective and irreversible BTK inhibitor with an IC₅₀ value of 1.95 nM. Poseltinib effectively suppressed splenic B220⁺GL7⁺, B220⁺CD138⁺, and B220⁺CD69⁺B cell counts, and anti-dsDNA IgG and reduced splenomegaly and lymph node enlargement. It also prevented skin lesions caused by lupus development, ameliorated renal inflammation and damage with increased blood urea nitrogen and creatinine, and decreased proteinuria. Furthermore, Poseltinib also decreased mortality from lupus development in both mouse models. Those results indicated that inhibition of BTK by Poseltinib effectively reduced B cell hyperactivity and significantly attenuated the development of SLE (Systemic lupus erythematosus) and LN (lupus nephritis) in rodent SLE models.
作用机制Poseltinib may covalently bind to the active site (cysteine 481 residue) of BTK.