中文名称 | Tazemetostat (EPZ-6438; E-7438) | 他泽司他 |
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英文名称 | Tazemetostat (EPZ-6438; E-7438) |
CAS号 | 1403254-99-8 |
分子式 | C34H44N4O4 |
分子量 | 572.74 |
外观 | Off-white to light yellow powder |
储存条件 | Dry, dark and at 0 - 4 ℃ for short term (days to weeks) or -20 ℃ for long term (months to years). |
Tazemetostat, also known as EPZ-6438 and E7438, is a potent, selective, and orally bioavailable small-molecule inhibitor of EZH2 enzymatic activity. EPZ-6438 induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells. Treatment of xenograft-bearing mice with EPZ-6438 leads to dose-dependent regression of MRTs with correlative diminution of intratumoral trimethylation levels of lysine 27 on histone H3, and prevention of tumor regrowth after dosing cessation.
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