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Tazemetostat trihydrochloride is a selective and orally available inhibitor of EZH2 (IC50: 4 nM for rat EZH2). It inhibits the activity of human PRC2-containing wild-type EZH2 (Ki: 2.5 nM). It inhibits EZH2 (IC50s: 11 and 16 nM in peptide assay and nucleosome assay).
Tazemetostat trihydrochloride is a selective and orally available inhibitor of EZH2 (IC50: 4 nM for rat EZH2). It inhibits the activity of human PRC2-containing wild-type EZH2 (Ki: 2.5 nM). It inhibits EZH2 (IC50s: 11 and 16 nM in peptide assay and nucleosome assay).
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
100 mg | 询价 | 期货 | |
500 mg | 询价 | 期货 |
产品描述 | Tazemetostat trihydrochloride is a selective and orally available inhibitor of EZH2 (IC50: 4 nM for rat EZH2). It inhibits the activity of human PRC2-containing wild-type EZH2 (Ki: 2.5 nM). It inhibits EZH2 (IC50s: 11 and 16 nM in peptide assay and nucleosome assay). |
靶点活性 | EZH2 (WT):2.5 nM (ki), EZH2:11 nM (in peptide assay), EZH2:16 nM (in nucleosome assay), EZH2 (rat):4 nM, EZH1:392 nM |
体外活性 | Tazemetostat inhibits multi wild-type and mutant lymphoma cell lines proliferation (IC50s: 0.49 nM-7.6 μM). |
体内活性 | Tazemetostat (250 or 500 mg/kg twice daily for 21-28 days) almost removes the fast-growing G401 tumors. |
别名 | EPZ-6438 trihydrochloride, E-7438 trihydrochloride |
分子量 | 682.12 |
分子式 | C34H47Cl3N4O4 |
CAS No. | 1403255-00-4 |
密度 | no data available |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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