上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。
Tazemetostat trihydrochloride (Synonyms: EPZ-6438 trihydrochloride; E-7438 trihydrochloride)
Tazemetostat trihydrochloride (EPZ-6438 trihydrochloride) 是一种有效,选择性,口服的 EZH2 抑制剂。Tazemetostat trihydrochloride 抑制含有 PRC2 复合体的野生型 EZH2 的活性, Ki 值为 2.5 nM。Tazemetostat trihydrochloride 抑制 EZH2,在肽测定和核小体测定中 IC50 分别为 11 和 16 nM。Tazemetostat trihydrochloride 抑制大鼠 EZH2,IC50 为 4 nM。Tazemetostat trihydrochloride 还抑制 EZH1,IC50 为 392 nM。
Tazemetostat trihydrochloride Chemical Structure
CAS No. : 1403255-00-4
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Tazemetostat trihydrochloride 的其他形式现货产品:
生物活性 |
Tazemetostat trihydrochloride (EPZ-6438 trihydrochloride) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat trihydrochloride inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki of 2.5 nM. Tazemetostat trihydrochloride inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat trihydrochloride inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat (EPZ-6438) also inhibits EZH1 with an IC50 of 392 nM[1]. |
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IC50 & Target[1] |
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体外研究 (In Vitro) |
Tazemetostat (EPZ-6438) inhibits multi wild-type and mutant lymphoma cell lines proliferation with IC50s of 0.49 nM-7.6 μM[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation Assay[1]
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体内研究 (In Vivo) |
Tazemetostat (EPZ-6438; 250 or 500 mg/kg twice daily for 21-28 days) practically eliminates the fast-growing G401 tumors[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
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Clinical Trial |
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分子量 |
682.12 |
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Formula |
C34H47Cl3N4O4 |
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CAS 号 |
1403255-00-4 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis. |
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参考文献 |
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