Merck
All Photos(1)

SML0895

Sigma-Aldrich

AGI-6780

≥98% (HPLC)

Synonym(s):
N-Cyclopropyl-4-(3-thienyl)-3-[[[[3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-benzenesulfonamide
Empirical Formula (Hill Notation):
C21H18F3N3O3S2
CAS Number:
Molecular Weight:
481.51
NACRES:
NA.77

Nivel de calidad

100

ensayo

≥98% (HPLC)

formulario

powder

color

white to light brown

solubilidad

DMSO: 20 mg/mL, clear

temp. de almacenamiento

2-8°C

Envase

5, 25 mg in glass bottle

Acciones bioquímicas o fisiológicas

AGI-6780 is a selective inhibitor of IDH2/R140Q a tumor-associated mutant of isocitrate dehydrogenase IDH2. Several human cancers have somatic point mutations in the genes encoding isocitrate dehydrogenases 1 and 2 (IDH1 and IDH2), confering a gain-of-function in cancer cells in which the mutant enzymes produce the oncometabolite (R)-2-hydroxyglutarate, [(R)-2HG]. (R)-2HG inhibits histone- and DNA-modifying enzymes, resulting in altered gene expression, histone and DNA hypermethylation, and inducing a block in cellular differentiation that promotes tumorigenesis. AGI-6780 reduced (R)-2HG levels in cell lines overexpressing IDH2/R140Q with an EC50 of 20 nM, and induced differentiation of TF-1 erythroleukemia and primary human acute myelogenous leukemia cells in vitro. AGI-6780 binds allosterically at the dimer interface of IDH2. AGI-6780 shows good selectivity against other dehydrogenases, including the closely related IDH1-WT or R132H mutant enzymes.

Características y beneficios

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Código de clase de almacenamiento

13 - Non Combustible Solids

WGK

WGK 3

Punto de inflamabilidad F

Not applicable

Punto de inflamabilidad C

Not applicable

Certificate of Analysis

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Certificate of Origin

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