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| 品牌 | absin | CAS | 1355326-35-0 |
|---|---|---|---|
| 分子式 | C27H31FN4O2 | 纯度 | ＞98% |
| 分子量 | 462.56 | 货号 | abs810560 |
| 供货周期 | 现货 | 主要用途 | is the first highly potent and selective |
| 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
AGI5198 1355326-35-0
| 产品描述 | |
| 描述 | AGI-5198 is the first highly potent and selective inhibitor of IDH1 R132H/R132C mutants with IC50 of 0.07 μM/0.16 μM. |
| 纯度 | >98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | IDH-C35,AGI5198,AGI 5196 |
| 外观 | Powder |
| 可溶性/溶解性 | DMSO 24 mg/mL (51.88 mM) Ethanol 14 mg/mL (30.26 mM) |
| 生物活性 | |
| 靶点 | Isocitrate Dehydrogenase (IDH) |
| In vitro(体外研究) | Measurements of R-2HG concentrations in pellets of TS603 glioma cells demonstrates dose-dependent inhibition of the mutant IDH1 enzyme by AGI-5198. AGI-5198 does not impair colony formation of two patient-derived glioma lines that express only the wild-type IDH1 allele (TS676 and TS516). Cancer cells heterozygous for the IDH1(R132H) mutation exhibits less IDH-mediated production of NADPH, such that after exposure to ionizing radiation (IR), there are higher levels of reactive oxygen species, DNA double-strand breaks, and cell death compared with IDH1 wild-type cells. These effects are reversed by the IDH1(R132H) inhibitor AGI-5198. |
| In vivo(体内研究) | AGI-5198 (450 mg/kg, p.o.) causes 50 to 60% growth inhibition of the tumor growth from human glioma xenografts. Tumors from AGI-5198- treated mice show reduced staining with an antibody against the Ki-67 protein. AGI-5198 does not affect the growth of IDH1 wild-type glioma xenografts. |
| 研究领域 | |
| 研究领域 | CancerCancer MetabolismMetabolic signaling pathwayMetabolism of lipids and lipoproteins MetabolismPathways and ProcessesMetabolic signaling pathwaysEnergy transfer pathwaysEnergy Metabolism MetabolismPathways and ProcessesMetabolic signaling pathwaysLipid and lipoprotein metabolismLipid metabolism NeuroscienceDevelopment NeuroscienceProcesses Signal TransductionMetabolismEnergy Metabolism Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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