EED226

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

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。

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.

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EED226 | EED-226 | EED 226

Others

Other Targets

EED| PRC2

Cancer

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2083627-02-3

369.4

C17H15N5O3S

>98% (HPLC)

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

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

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

(-20℃)

With Ice Pack

≥ 2 years