AGI6780

Data Sheet For research use only. Not for human use.

Cat. No. ：BCP07383CAS No. ：1432660-47-3Purity：98%

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CAS No.	1432660-47-3	Cat. No.	BCP07383
Name	AGI6780
Synonyms	AGI 6780; AGI-6780;
SMILES
Chemical Name
Formula	C21H18F3N3O3S2	M. Wt	481.51
Purity	98%	Storage	Store at 4-8°C
Description	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. 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).AGI-6780 is a potent, selective inhibitor of mutant IDH2 with an IC50 value of 23 nM. 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. In primary human acute myelogenous leukemia cells, AGI-6780 suppressed cell growth and induced differentiation of immature blast cells toward macrophage and granulocytic lineages.