MAK683( MAK-683 | MAK683 )

Catalog No. M13052 CAS No. 1951408-58-4

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

Get Quotation Bulk Inquiry Add to Cart

Product Name

MAK683
Note

Research use only, not for human use.
Brief Description

MAK683 (MAK-683) is a novel inhibitor of embryonic ectoderm development protein (EED) and allosteric inhibitor of polycomb repressive complex 2 (PRC2).
Description

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.
In Vitro

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

——
Synonyms

MAK-683 | MAK683
Pathway

Chromatin/Epigenetic
Target

HMTase
Recptor

HMTase
Research Area

Cancer
Indication

Blood cancer

CAS Number

1951408-58-4
Formula Weight

376.39
Molecular Formula

C20H17FN6O
Purity

>98% (HPLC)
Solubility

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
Chemical Name

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