AGI-5198, R132 mutant isocitrate dehydrogenase inhibitor

Product Details

Formal Name: N-[2-(Cyclohexylamino)-1-(2-methylphenyl)-2-oxoethyl]-N-(3-fluorophenyl)-2-methyl-1H-imidazole-1-acetamide

Molecular Formula: C₂₇H₃₁FN₄O₂

Formula Weight: 462.56

CAS Number: 1355326-35-0

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 10 mg/ml) or in Ethanol (up to 5 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

Applications

R132 mutant isocitrate dehydrogenase inhibitor

Functions

AGI-5198 is a potent (IC50 = 70 nM) inhibitor of mutant isocitrate dehydrogenase 1(IDH1). It is selective for the R132H-IDH1 mutant and does not affect wild type cells. This mutation results in loss-of-function for oxidative decarboxylation of isocitrate and gain-of-function for production of the oncometabolite R-2-hydroxyglutarate (R-2HG) form alpha-ketoglutarate (2-OG).

Application Procedures

First dissolved in DMSO (up to 10 mg/ml) or in Ethanol (up to 5 mg/ml), then diluted to aqueous buffer. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.

Research use only.

Documents

• Datasheet (PDF)
• MSDS (PDF)