Tazemetostat (EPZ-6438, E7438)是一种有效的，选择性EZH2抑制剂，无细胞试验中Ki 和 IC50分别为2.5 nM 和 11 nM，比作用于EZH1选择性高35倍，比作用于14种其他HMT选择性高4500多倍。 Information Tazemetostat (EPZ-6438) Tazemetostat (EPZ-6438, E7438) is a potent, and selective EZH2 inhibitor with K i and IC50 of 2.5 nM and 11 nM in cell-free assays, exhibiting a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other HMTs. Targets EZH2 (Cell-free assay) 2.5 nM(Ki) In vitro EPZ-6438 concentration-dependently reduces global H3K27Me3 levels in wild-type or SMARCB1 mutant cells, and induces strong antiproliferative effects with IC50 ranging from 32 nM to 1000 nM in SMARCB1-deleted MRT cell lines. EPZ-6438 induces gene expression of neuronal differentiation and cell cycle inhibition, while inhibtis expression of Hedgehog pathway genes, MYC and EZH2. The antiproliferative effect of EPZ-6438 is enhanced by either prednisolone or dexamethasone in several EZH2 mutant lymphoma cell lines. In vivo In SCID mice bearing s.c. G401 xenografts, EPZ-6438 induces tumor stasis during the administration period and produces a significant tumor growth delay with minimal effect on body weight. Cell Research(from reference) Cell lines：Mutant cell lines (G401, A204, G402, KYM-1), Wild type cell line (RD, 293, SJCRH30) Concentrations：~10 μM Incubation Time：7 days
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Tazemetostat (EPZ-6438)
Dangerous GoodsCAS number：1403254-99-8 molecular formula：C34H44N4O4
overview
compound introduction
Specs
| Chinese alias | 他泽司他(EPZ-6438) | ||
| English alias | HMS3653O07 | Tazemetostat [USAN:INN] | Tazemetostatum | BCP07409 | HMS3747A09 | SW220030-1 | 5-(Ethyl(tetrahydro-2H-pyran-4-yl)amino)-N-((2-hydroxy-4,6-dimethylpyridin-3-yl)methyl)-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide | N-[(4,6-Dim | ||
| CAS number | 1403254-99-8 | molecular formula | C34H44N4O4 |
| molecular weight | 572.74 g/mol | Exact mass | - |
| PSA | 83.100 Ų | logp | 3.506 |
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physicochemical properties
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Safety information
pictogram：
GHS07
Signal word：
Warning
Hazard Statement：
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激 H302: 吞食有害
Statement of Preventive Measures：
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。
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