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

Chemical Structure : Pinometostat

CAS No.: 1380288-87-8

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Pinometostat (EPZ-5676, EPZ5676)

货号: PC-21618Not For Human Use, Lab Use Only.

Pinometostat (EPZ-5676) is a potent and selective inhibitor of DOT1L histone methyltransferase activity with Ki of 0.08 nM, 37000-fold selectivity over other methyltransferases.

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10 mg ￥1580 In stock
25 mg ￥2680 In stock
50 mg ￥4280 In stock
100 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

Pinometostat (EPZ-5676) is a potent and selective inhibitor of DOT1L histone methyltransferase activity with Ki of 0.08 nM, 37000-fold selectivity over other methyltransferases.
EPZ-5676 occupies the S-adenosyl methionine (SAM) binding pocket and induces conformational changes in DOT1L.
Pinometostat (EPZ-5676) potently inhibits cellular H3K79 methylation with IC50 of 3 nM and 5 nM in MV4-11 and HL60 (non–MLL-rearranged) cells, respectively, inhibits MLL-fusion target gene expression.
Pinometostat (EPZ-5676) selectively inhibits proliferation of MLL-rearranged leukemia cells with IC50 of 3.5 nM (MV4-11 proliferation), demonstrates nanomolar antiproliferative activity against most of the MLL-rearranged cell lines, but not non-MLL-rearranged cell lines.
EPZ-5676 (70 mg/kg) causes complete and sustained regression in rodent subcutaneous (SC) MV4-11 xenograft models.

物理化学性质&存储条件

分子量 562.72
分子式 C30H42N8O3
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

(2R,3R,4S,5R)-2-(6-Amino-9H-purin-9-yl)-5-(((cis-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol

参考文献

1. Daigle SR, et al. Blood. 2013 Aug 8;122(6):1017-25.

2. Klaus CR, et al. J Pharmacol Exp Ther. 2014 Sep;350(3):646-56.

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