Description:
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.
- Molecular Weight: 376.395
- Molecular Formula: C20H17FN6O
Purity: 98%
Canonical SMILES:
CC1=C(C=CC=N1)C2=CN=C(N3C2=NN=C3)NCC4=C(C=CC5=C4CCO5)F
InChI:
InChI=1S/C20H17FN6O/c1-12-13(3-2-7-22-12)16-10-24-20(27-11-25-26-19(16)27)23-9-15-14-6-8-28-18(14)5-4-17(15)21/h2-5,7,10-11H,6,8-9H2,1H3,(H,23,24)
InChIKey: XLIBABIFOBYHSV-UHFFFAOYSA-N
- Solubility: Soluble in DMSO.
- Appearance: Solid Powder
Synonyms:
MAK-683; MAK 683; MAK683; EED inhibitor-1; 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
More details are to be found on supplier website
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