EED226 ( EED226 | EED-226 | EED 226 )

产品货号. M17425 CAS No. 2083627-02-3

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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产品名称

EED226
注意事项

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
产品简述

EED226 是一种有效的、选择性的、口服生物可利用的胚胎外胚层发育 (EED) 抑制剂，IC50 为 22 nM。
产品描述

EED226 is a potent, selective, and orally bioavailable EED inhibitor. induces robust and sustained tumor regression in EZH2MUT preclinical DLBCL model. EED226 induces a conformational change upon binding EED, leading to loss of PRC2 activity. EED226 shows similar activity to SAM-competitive inhibitors in blocking H3K27 methylation of PRC2 target genes and inducing regression of human lymphoma xenograft tumors. Interestingly, EED226 also effectively inhibits PRC2 containing a mutant EZH2 protein resistant to SAM-competitive inhibitors. EED226 inhibits PRC2 activity via an allosteric mechanism and offers an opportunity for treatment of PRC2-dependent cancers. demonstrated very impressive antitumor activities in mouse xenograft model.
体外实验

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体内实验

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同义词

EED226 | EED-226 | EED 226
通路

Others
靶点

Other Targets
受体

EED| PRC2
研究领域

Cancer
适应症

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CAS Number

2083627-02-3
分子量

369.4
分子式

C17H15N5O3S
纯度

>98% (HPLC)
溶解度

DMSO : ≥ 29 mg/mL. 78.51 mM; H2O : < 0.1 mg/mL
SMILES

c1(n2c(c(cn1)c1ccc(cc1)S(=O)(=O)C)nnc2)NCc1occc1
化学全称

N-(Furan-2-ylmethyl)-8-(4-(methylsulfonyl)phenyl)[1,2,4]-triazolo[4,3-c]pyrimidin-5-amine

1.Huang Y, et al. J Med Chem. 2017 Mar 23;60(6):2215-2226.

计算器

产品手册

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