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| Product Name | IDH1 Inhibitor, R132 Somatic Mutant-Specific, AGI-5198 |
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| Description | Purity ~98% (HPLC). A cell-permeable phenyl-glycine analog that acts as an IDH1 (Isocitrate Dehydrogenase 1) R132 somatic mutant-specific inhibitor (IC50 = 0.07, 0.16, and >100uM, respectively, against R132H, R132C, and wt IDH1), potently inhibiting oncometabolite 2-HG (D-2-hydroxyglutarate) production, but not cancer viability, in R132H-harboring U87-MG glioblastoma and R132C-harboring HT1080 chondrosarcoma cultures in vitro (IC50 = 70 and 480nM, respectively; 48h) and in R132H U87-MG tumor-bearing mice in vivo (150mg/kg/12h i.p.). Oncometabolite 2-HG acts as an alpha-KG-competitive inhibitor against multiple alpha-KG-dependent enzymes that are important in maintaining normal cellular functions, including epigenetic regulations. Formula: C27H31FN4O BULL; HCl Solubility: DMSO or H2O Primary Target: active site IDH1 mutant homodimer Primary Target IC50: 0.07, 0.16, and > Molar Mass: 490 |
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| Size | 25mg |
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| Concentration | n/a |
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| Applications | n/a |
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| Other Names | IDH1 Inhibitor, R132 Somatic Mutant-Specific, AGI-5198 (Isocitrate Dehydrogenase 1 R132 Somatic Mutant Inhibitor, AGI-5198, N-Cyclohexyl-2-(N-(3-fluorophenyl)-2-(2-methyl-1H-imidazol-1-yl)acetamido)-2-(o-tolyl)acetamide, HCl, AGI-5198, AGI-5198) |
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| Gene, Accession, CAS # | n/a |
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| Catalog # | 217450 |
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| Order / More Info | IDH1 Inhibitor, R132 Somatic Mutant-Specific, AGI-5198 from UNITED STATES BIOLOGICAL |
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| Product Specific References | n/a |
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