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产品描述 |
Tazemetostat, also known as EPZ-6438 and E7438, is a potent, selective, and orally bioavailable small-molecule inhibitor of EZH2 enzymatic activity. EPZ-6438 induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells. Treatment of xenograft-bearing mice with EPZ-6438 leads to dose-dependent regression of MRTs with correlative diminution of intratumoral trimethylation levels of lysine 27 on histone H3, and prevention of tumor regrowth after dosing cessation. These data demonstrate the dependency of SMARCB1 mutant MRTs on EZH2 enzymatic activity and portend the utility of EZH2-targeted drugs for the treatment of these genetically defined cancers. |
化学结构 |
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化学名称 |
N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide |
SMILES Code |
O=C(C1=CC(C2=CC=C(CN3CCOCC3)C=C2)=CC(N(CC)C4CCOCC4)=C1C)NCC5=C(C)C=C(C)NC5=O |
基本信息 |
产品编号:XM173 产品名称:EPZ-6438 (Tazemetostat) 别名:EPZ-6438; EPZ 6438; EPZ6438; E7438; E-7438; E 7438; Tazemetostat CAS#:1403254-99-8 分子式:C34H44N4O4 精确分子量:572.33626 分子量:572.74
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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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