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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 |
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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%
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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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