AGI6780

参考资料仅供科学研究，不可用于个人用途。

货号：BCP07383CAS号：1432660-47-3纯度：98%

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CAS号	1432660-47-3	货号	BCP07383
中文名	AGI6780
英文名	AGI6780
中文别名
英文别名	AGI 6780; AGI-6780;
SMILES
化学名称
分子式	C21H18F3N3O3S2	分子量	481.51
纯度	98%	配送	惯例下常温包邮
产品描述	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.