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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) |
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. |
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.
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. |
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 |
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