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| | N-cyclohexyl-2-(N-(3-fluorophenyl)-2-(2-Methyl-1H-iMidazol-1-yl)acetaMido)-2-(o-tolyl)acetaMide Basic information |
| | N-cyclohexyl-2-(N-(3-fluorophenyl)-2-(2-Methyl-1H-iMidazol-1-yl)acetaMido)-2-(o-tolyl)acetaMide Chemical Properties |
| Boiling point | 707.6±60.0 °C(Predicted) | | density | 1.21±0.1 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | DMSO: soluble3mg/mL, clear | | form | powder | | pka | 14.02±0.20(Predicted) | | color | white to beige | | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. | | InChIKey | FNYGWXSATBUBER-UHFFFAOYSA-N |
| Hazard Codes | T | | Risk Statements | 25 | | Safety Statements | 45 | | RIDADR | UN 2811 6.1 / PGIII | | WGK Germany | 3 |
| | N-cyclohexyl-2-(N-(3-fluorophenyl)-2-(2-Methyl-1H-iMidazol-1-yl)acetaMido)-2-(o-tolyl)acetaMide Usage And Synthesis |
| Description | AGI-5198 (135526-35-0) is a potent (IC50?= 70 nM) inhibitor of mutant isocitrate dehydrogenase 1(IDH1).1? It is selective for the R132H-IDH1 mutant and does not affect wild type cells.2? 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) from alpha-ketoglutarate (2-OG). | | Uses | AGI5198 inhibits mutant IDH1 (isocitrate dehydrogenase 1) in cancer cells which delays growth and promotes differentiation of the glioma cells. | | Uses | AGI-5198 has been used as a negative control in ligand dilution series. | | Biochem/physiol Actions | In human chondrosarcoma cell line JJ012, AGI-5198 promotes apoptosis and G2/M cell cycle arrest. It also prevents the generation of colony in chondrosarcoma cell lines. AGI-5198 hinders the multiplication of cell and induces demethylation of H3K9me3 and H3K27me3. | | target | R132H-IDH1 | | storage | Store at -20°C | | References | 1) Popovici-Muller?et al. (2012),?Discovery of the First Potent Inhibitors of Mutant IDH1 That Lower Tumor 2-HG In Vivo; ACS Med. Chem. Lett.,?3?850
2) Rohle?et al. (2013),?An inhibitor of mutant IDH1 delays growth and promotes differentiation of glioma cells; Science,?340?626 |
| | N-cyclohexyl-2-(N-(3-fluorophenyl)-2-(2-Methyl-1H-iMidazol-1-yl)acetaMido)-2-(o-tolyl)acetaMide Preparation Products And Raw materials |
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