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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-EPZ004777
EPZ004777

Chemical Structure : EPZ004777

CAS No.: 1338466-77-5

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EPZ004777 (EPZ 004777)

货号: PC-21619Not For Human Use, Lab Use Only.

EPZ004777 is a potent, selective inhibitor of DOT1L with Ki of 0.3 nM and IC50 of 0.4 nM, selectively inhibits H3K79 methylation and blocks expression of leukemogenic genes.

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10 mg ￥1580 In stock
25 mg ￥2680 In stock
50 mg ￥4280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

EPZ004777 is a potent, selective inhibitor of DOT1L with Ki of 0.3 nM and IC50 of 0.4 nM, selectively inhibits H3K79 methylation and blocks expression of leukemogenic genes.
EPZ004777 displays remarkable selectivity (>1000-fold) for inhibition of DOT1L over other histone methyltransferases (HMTs).
EPZ004777 selectively inhibits cellular H3K79 methylation, does not change the methylation state of residues targeted by PRDM and SMYD family members (H3K9 and H3K4, respectively)
EPZ004777 inhibits expression of key MLL fusion target genes, HOXA9 and MEIS1.
EPZ004777 selectively inhibits proliferation of MLL-Rearranged cell lines and MLL-AF9-transformed murine hematopoietic cells (RS4;11, MLL-AF4, IC50=6.47 nM).
EPZ004777 significantly decrease H3K79me2 levels and exhibits antitumor efficacy in mouse xenograft model of MLL.

物理化学性质&存储条件

分子量 539.68
分子式 C28H41N7O4
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

1-(3-((((2R,3S,4R,5R)-5-(4-Amino-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl)(isopropyl)amino)propyl)-3-(4-(tert-butyl)phenyl)urea

参考文献

1. Daigle SR, et al. Cancer Cell. 2011 Jul 12;20(1):53-65.

2. Chen L, et al. Leukemia. 2013 Apr;27(4):813-22.

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