MAK683 ( MAK-683 | MAK683 )

产品货号. M13052 CAS No. 1951408-58-4

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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产品名称

MAK683
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

MAK683 (MAK-683) 是一种新型胚胎外胚层发育蛋白 (EED) 抑制剂和多梳抑制复合物 2 (PRC2) 的变构抑制剂。
产品描述

MAK683 (MAK-683) is a novel inhibitor of embryonic ectoderm development protein (EED) and allosteric inhibitor of polycomb repressive complex 2 (PRC2), selectively binds to the domain of EED that interacts with H3K27me3; leads to a conformational change in the EED H3K27me3-binding pocket and prevents the interaction of EED with the histone methyltransferase enhancer zeste homolog 2 (EZH2), inhibits tumor cell proliferation in EZH2-mutated and PRC2-dependent cancer cells.Blood Cancer Phase 2 Clinical(In Vitro):MAK683 has antiproliferative activities in B cell lymphoma cell KARPAS422 after 14 days of treatment with an IC50 of 30 nM.
体外实验

MAK683 has antiproliferative activities in B cell lymphoma cell KARPAS422 after 14 days of treatment with an IC50 of 30 nM.
体内实验

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同义词

MAK-683 | MAK683
通路

Chromatin/Epigenetic
靶点

HMTase
受体

HMTase
研究领域

Cancer
适应症

Blood cancer

CAS Number

1951408-58-4
分子量

376.39
分子式

C20H17FN6O
纯度

>98% (HPLC)
溶解度

DMSO : 52 mg/mL 138.15 mM; H2O : < 0.1 mg/mL
SMILES

CC1=C(C=CC=N1)C2=CN=C(N3C2=NN=C3)NCC4=C(C=CC5=C4CCO5)F
化学全称

N-[(5-fluoro-2,3-dihydro-1-benzofuran-4-yl)methyl]-8-(2-methylpyridin-3-yl)-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine