EPZ6438
货号：
16174-50mg 基本售价：
8582.0 元 规格：
50 mg
产品信息
概述| 货号 | 16174-50mg |
| 描述 | EPZ6438 is an orally bioavailable, selective inhibitor of the lysine methyltranferase EZH2 (Ki = 2.5 nM), the enzymatic subunit of polycomb repressive complex 2.1 It displays a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other histone methyltransferases.1 EPZ6438 blocks histone H3 lysine 27 trimethylation in both wild-type and mutant lymphoma cells (IC50s range from 2-90 nM).2 EPZ6438 has been shown to induce apoptosis and differentiation specifically in SMARCB1-deleted malignant rhabdoid tumor cells and to promote their regression in xenograft-bearing mice.1 |
| 别名 | Tazemetostat; |
性能| 供应商 | Cayman |
| 应用文献 |
1.Knutson, S.K.,Warholic, N.M.,Wigle, T.J., et al. Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2. Proceedings of the National Academy of Sciences of the United States of America 110(19), 7922-7927 (2013).
2.Knutson, S.K.,Kawano, S.,Minoshima, Y., et al. Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma. Molecular Cancer Therapeutics 13(4), 842-854 (2014).
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| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 572.7 |
| 分子式 | C34H44N4O4 |
| CAS号 | 1403254-99-8 |
| 稳定性 | ≥ 2 years |
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