AGI-6780

AGI-6780

Biochem/physiol Actions

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.

Features and Benefits

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Packaging

5, 25 mg in glass bottle

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Code Description Colour Quality Level Manufacturer Storage Temp. Solubility Form Assay Price Quantity
3574212 AGI-6780 white to light brown 100 SIGMA-ALDRICH 2-8°C DMSO: 20 mg/mL, clear powder ≥98% (HPLC)
£518.14 (exc VAT) per 25MG
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3574213 AGI-6780 white to light brown 100 SIGMA-ALDRICH 2-8°C DMSO: 20 mg/mL, clear powder ≥98% (HPLC)
£206.14 (exc VAT) per 5MG
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