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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-Tazemetostat
Tazemetostat

Chemical Structure : Tazemetostat

CAS No.: 1403254-99-8

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Tazemetostat (EPZ-6438, E-7438)

货号: PC-21938Not For Human Use, Lab Use Only.

Tazemetostat (EPZ-6438) is a potent, selective, SMA-competitive and orally available EZH2 inhibitor with IC50 of 11 and 16 nM in peptide assay and nucleosome assay, respectively.

规格 价格 库存 数量
10 mg ￥580 In stock
25 mg ￥980 In stock
50 mg ￥1480 In stock
100 mg ￥2180 In stock
250 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Tazemetostat (EPZ-6438) is a potent, selective, SMA-competitive and orally available EZH2 inhibitor with IC50 of 11 and 16 nM in peptide assay and nucleosome assay, respectively.
Tazemetostat (EPZ-6438) inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with Ki of 2.5 nM, inhibits rat EZH2 with IC50 of 4 nM.
Tazemetostat (EPZ-6438) selectively inhibits intracellular lysine 27 of histone H3 (H3K27) methylation in a concentration- and time-dependent manner in both EZH2 wild-type and mutant lymphoma cells.
Tazemetostat (EPZ-6438) treatment causes dose-dependent tumor growth inhibition in EZH2-mutant NHL xenograft-bearing mice.

物理化学性质&存储条件

分子量 572.75
分子式 C34H44N4O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-((4,6-Dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide

参考文献

1. Knutson SK, et al. Mol Cancer Ther. 2014 Apr;13(4):842-54.

2. Knutson SK, et al. PLoS One. 2014 Dec 10;9(12):e111840.

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