生物活性
EPZ-6438 (Tazemetostat)是一种有效的，选择性的，口服可利用的EZH2酶促活性小分子抑制剂，无细胞试验中Ki 和 IC50分别为2.5 nM 和 11 nM。它诱导SMARCB1缺失的MRT细胞中的凋亡和分化。
靶点信息
| EZH2 (Cell-free assay) | EZH2 (Cell-free assay) | | | |
| 2.5 nM(Ki) | 2.5 nM(Ki) | | | |
化学数据
| 目录号 | A12712 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 572.74 |
| Formula | C34H44N4O4 |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for36 months.
In solution, store at -20ºC and use within3 monthsto prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles. |
| CAS No. | 1403254-99-8 |
| Synonyms | EPZ6438, EPZ 6438 |
| SMILES | CCN(C1CCOCC1)C2=CC(=CC(=C2C)C(=O)NCC3=C(C=C(NC3=O)C)C)C4=CC=C(C=C4)CN5CCOCC5 |
溶解度
| In vitro (25°C) | DMSO | Warmed: 4 mg/mL (6.98 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 4% DMSO+30% PEG 300+5% Tween 80+ddH2O | 2.3 mg/mL |
*<1 mg/ml means slightly soluble or insoluble.
*Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 17.46 mL | 87.3 mL | 174.6 mL |
| 0.5 mM | 3.49 mL | 17.46 mL | 34.92 mL |
| 1 mM | 1.75 mL | 8.73 mL | 17.46 mL |
| 5 mM | 0.35 mL | 1.75 mL | 3.49 mL |
*The above data is based on the productmolecular weight 572.74. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
