A potent

AGI-6780 – 1 mg

Brand:
Cayman
CAS:
1432660-47-3
Storage:
-20
UN-No:
Non-Hazardous - /

Isocitrate dehydrogenases (IDHs) are NAD+ and NADP+-dependent enzymes in the tricarboxylic acid cycle that catalyze oxidative decarboxylation of isocitrate producing α-ketoglutarate (2-OG) and carbon dioxide. IDH1 and IDH2 are mutated in >70% of lower grade gliomas.{22138} The most common mutations map to arginine residues in the catalytic pockets of IDH1 (R132) or IDH2 (R140 and R172) and impart new gain of function catalytic activity leading to the NADPH-dependent conversion of 2-OG to 2-hydroxyglutarate (2-HG).{22135,22156,20681} AGI-6780 is a potent, selective inhibitor of mutant IDH2 with an IC50 value of 23 nM.{23425} It binds allosterically at the dimer interface of mutant IDH2-R140Q, inhibiting 2-HG formation in human glioblastoma U87 and TF-1 cells expressing IDH2-R140Q with IC50 values of 11 and 18 nM, respectively.{23425} In primary human acute myelogenous leukemia cells, AGI-6780 suppressed cell growth and induced differentiation of immature blast cells toward macrophage and granulocytic lineages.{23245}  

 

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Description

A potent, selective inhibitor of mutant IDH2 (IC50 = 23 nM) that inhibits 2-HG formation in human glioblastoma U87 and TF-1 cells expressing IDH2-R140Q (IC50s = 11 and 18 nM, respectively); suppresses cell growth of primary human AML cells and induces differentiation of immature blast cells towards macrophage and granulocytic lineages

Formal name: N-cyclopropyl-4-(3-thienyl)-3-[[[[3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-benzenesulfonamide

Synonyms: 

Molecular weight: 481.5

CAS: 1432660-47-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Metabolism

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