MAK683 Cas:1951408-58-4

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Product Description:

Product Name: MAK683 CAS NO: 1951408-58-4

 

Synonyms:

N-[(5-Fluoro-2,3-dihydro-4-benzofuranyl)methyl]-8-(2-methyl-3-pyridinyl)-1,2,4-triazolo[4,3-c]pyrimidin-5-amine;

1,2,4-Triazolo[4,3-c]pyrimidin-5-amine, N-[(5-fluoro-2,3-dihydro-4-benzofuranyl)methyl]-8-(2-methyl-3-pyridinyl)-;

 

Chemical & Physical Properties:

Appearance: Solid or powder

Assay :≥98.0%

Density: 1.47±0.1 g/cm3 (Predicted)

PKa: 2.70±0.12 (Predicted)

Solubility: Soluble in DMSO.

 

EED inhibitor-1 is an EED inhibitor extracted from patent US20160176882 A1, compound example 2; has IC50s of 59, 89, 26 nM in EED Alphascreen binding, LC-MS and ELISA assay. MAK683 is an inhibitor of embryonic ectoderm development protein (EED) with potential antineoplastic activity. MAK683 binds to the domain of EED that interacts with trimethylated lysine 27 on histone 3 (H3K27me3), leading to a conformational change in the EED H3K27me3-binding pocket and preventing the interaction of EED with the histone methyltransferase enhancer zeste homolog 2 (EZH2). MAK683 is undergoing phase II clinical trials for the identification of antitumor activity.

 

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Products under patent are offered for R & D purpose only. However, the final responsibility lies exclusively with the buyer.

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