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AdipoGen AGI-5198 (25 mg)
Supplier: AdipoGen AGCR13528M025
Chemical. CAS: 1355326-35-0. Formula: C27H31FN4O2. MW: 462.6. Synthetic. Potent and selective inhibitor of IDH1 (isocitrate dehydrogenase 1) R132H and R132C mutants in vitro with IC50 values of 0.07 and 0.16 µM, respectively. Does not inhibit wild-type IDH1 or any of the examined IDH2 isoforms (IC50 > 100 µM). Isocitrate dehydrogenases (IDHs) are nicotinamide adenine dinucleotide (NAD+) and NAD phosphate (NADP+)-dependent enzymes in the tricarboxylic acid cycle that catalyze oxidative decarboxylation of isocitrate producing alpha-ketoglutarate (2-OG) and carbon dioxide. IDH1 and IDH2 are mutated in >70% of lower grade gliomas. Shown to have anti-tumor efficacy in the TS603 glioma cell line and to reduce tumor 2-HG production in HT1080 and U87MG cells. Caused 50-60% growth inhibition over a treatment period of three weeks with no affect in the growth of IDH1 wild-type glioma xenografts in R132H-IDH1 glioma xenografts.
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