MAK-683


Catalog No. size PriceQuantity
M7137-2 2mg solid $128
M7137-10 10mg solid $441

Description

Cas:1951408-58-4

Product Information

MAK-683 is a potent inhibitor of embryonic ectoderm development protein (EED) and allosteric inhibitor of polycomb repressive complex 2 (PRC2), with potential antineoplastic activity. Upon administration, MAK683 selectively binds to the domain of EED that interacts with trimethylated lysine 27 on histone 3 (H3K27me3), which 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).

 

Chemical Formula: C20H17FN6O

 

Exact Mass: 376.1448

 

Molecular Weight: 376.3954

 

Elemental Analysis: C, 63.82; H, 4.55; F, 5.05; N, 22.33; O, 4.25

 

Synonym:

 

MAK-683

MAK 683

MAK683

EED inhibitor-1

EED inhibitor 1

EED inhibitor1

 

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

 

InChi Key: 

XLIBABIFOBYHSV-UHFFFAOYSA-N

 

InChi Code: 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)

 

Smiles Code:

CC1=NC=CC=C1C2=CN=C(NCC3=C(F)C=CC4=C3CCO4)N5C2=NN=C5

Technical Data:

 

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

 

References

 

  1. Chan, Ho Man, et al. TRIAZOLOPYRIMIDINE COMPOUNDS AND USES THEREOF. US20160176882 A1.

 

  1. Huang D, et al. Binding Modes of Small-Molecule Inhibitors to the EED Pocket of PRC2. Chemphyschem. 2020 Feb 4;21(3):263-271.

 

Products are for research use only. Not for human use.

 

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