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产品类别
  活性分子
  抗癌类
  抗血栓类
  丙肝类
  风湿类
  糖尿病类
  神经系统类
  其他
  中间体
  特色产品
  其他

产品介绍
产品描述
ARQ 531 is an investigational, orally bioavailable, potent and reversible inhibitor of both wild type and C481S-mutant Bruton’s tyrosine kinase (BTK).B-cell malignancies, like chronic lymphocytic lymphoma (CLL), Waldenstrom’s macroglobulinemia, diffuse large B-cell lymphoma (DLBCL) and mantle cell lymphoma (MCL) are driven by BTK. The only approved BTK inhibitor, ibrutinib, is irreversible and makes a covalent bond with the C481 residue of the targeted protein. Although ibrutinib has demonstrated excellent responses in patients with elevated BCR signaling, clinical resistance has been observed, and the BTK-C481S mutation is emerging as a predominant mechanism of resistance. As a reversible inhibitor, ARQ 531 does not require interaction with the C481 residue, a binding site essential for irreversible ibrutinib binding to BTK, thus positioning ARQ 531 as a targeted therapy for CLL, DLBCL, MCL patients harboring C481S-mutant BTK who have developed resistance to irreversible BTK inhibitors. 
化学结构
 
化学名称
(2-Chloro-4-phenoxyphenyl)(4-(((3R,6S)-6-(hydroxymethyl)tetrahydro-2H-pyran-3-yl)amino)-7H-pyrrolo(2,3-d)pyrimidin-5-yl)methanone 
基本信息
产品编号:XM727 
产品名称:ARQ-531 
别名:ARQ531 
CAS#:2095393-15-8 
分子式:C25H23ClN4O4 
精确分子量:478.14 
分子量:478.93 
纯度:>98% 
物化性质

外观: 固体粉末

纯度: >98%

运输信息: 非危险化学品,适于常温或冰袋运输。

储存条件: 低温,干燥,避光。

溶解性:   溶于DMSO, 不溶于水

储存期限:3年 -20℃固体储存

         2 年  -80℃ 溶液储存

 



该产品只供科研使用,不能给病人提供。

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