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别名 氢溴酸泰泽司他, EPZ-6438 hydrobromide, E-7438 hydrobromide
Tazemetostat hydrobromide (E-7438 hydrobromide) 是口服的EZH2选择性抑制剂。它抑制含有 PRC2 复合体的野生型 EZH2 的活性,Ki 为 2.5 nM。它还抑制 EZH1,IC50为 392 nM。

Tazemetostat hydrobromide (E-7438 hydrobromide) 是口服的EZH2选择性抑制剂。它抑制含有 PRC2 复合体的野生型 EZH2 的活性,Ki 为 2.5 nM。它还抑制 EZH1,IC50为 392 nM。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 2 mg | ¥ 348 | In Stock | |
| 5 mg | ¥ 497 | In Stock | |
| 10 mg | ¥ 777 | In Stock | |
| 25 mg | ¥ 1,390 | In Stock | |
| 50 mg | ¥ 1,850 | In Stock | |
| 100 mg | ¥ 3,110 | In Stock | |
| 200 mg | ¥ 4,570 | In Stock | |
| 500 mg | ¥ 7,260 | In Stock | |
| 1 mL x 10 mM (in DMSO) | ¥ 877 | In Stock |
Tazemetostat hydrobromide 相关产品
| 产品描述 | Tazemetostat hydrobromide (E-7438 hydrobromide) is a potent and selective EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 (Ki: 2.5 nM). Tazemetostat hydrobromide also inhibits EZH1 (IC50: 392 nM). |
| 靶点活性 | EZH2:11 nM (in peptide assay), EZH2:16 nM (in nucleosome assay), EZH2 (rat):4 nM, EZH2 (WT):2.5 nM (Ki), EZH1:392 nM |
| 体外活性 | Tazemetostat hydrobromide 抑制大鼠EZH2,其IC50为4 nM。在肽检测和核小体检测中,Tazemetostat hydrobromide分别以IC50为11 nM和16 nM抑制EZH2。此外,Tazemetostat hydrobromide还能抑制多种野生型及突变型淋巴瘤细胞系增殖,其IC50范围从0.49 nM至7.6 μM [1]。 |
| 体内活性 | Tazemetostat(每日两次,每次250或500 mg/kg,连续21-28天)实际上可以彻底清除快速生长的G401肿瘤[1]。 |
| 别名 | 氢溴酸泰泽司他, EPZ-6438 hydrobromide, E-7438 hydrobromide |
| 分子量 | 653.65 |
| 分子式 | C34H45BrN4O4 |
| CAS No. | 1467052-75-0 |
| Smiles | O=C(C1=CC(C2=CC=C(CN3CCOCC3)C=C2)=CC(N(CC)C4CCOCC4)=C1C)NCC5=C(C)C=C(C)NC5=O.[H]Br |
| 密度 | 1.31g/cm3 |
| 颜色 | White |
| 物理性状 | Solid |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 100 mg/mL (152.99 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
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