产品说明书
IDH1 Inhibitor 8
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同义名 : | AG-120;racemic |
| CAS号 : | 1448346-63-1 | |
| 货号 : | A145388 | |
| 分子式 : | C28H22ClF3N6O3 | |
| 纯度 : | 99%+ | |
| 分子量 : | 582.961 | |
| MDL号 : | MFCD29044889 | |
| 存储条件： |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Isocitrate dehydrogenases (IDHs) catalyze the oxidative decarboxylation of isocitrate to 2-oxoglutarate. IDH1 is a NADP(+)-dependent isocitrate dehydrogenase found in the cytoplasm and peroxisomes. IDH1 serves a significant role in cytoplasmic NADPH production. Somatic mutations in IDH1 have recently been identified in multiple human cancers. Mutation at the site of R132 of IDH1 confer on this enzymes a new activity: catalysis of alpha-ketoglutarate (2-OG) to the (R)-enantiomer of 2-hydroxyglutarate (R-2HG). AG-120 Racemate is the racemate form of AG-120. AG-120 is a selective inhibitor of R132 mutated IDH1. The inhibitory IC50s of AG-120 against IDH1-R132 mutants IDH1-R132H, IDH1-R132C, IDH1-R132G, IDH1-R132L and IDH1-R132S were 12, 13, 8, 13, and 12 nM, respectively. The inhibitory IC50s of AG-120 against IDH1-R132 mutated HT1080, COR-L105 and HCCC-9810 cells were 8, 15 and 12 nM, respectively[3]. In IDH1-R132 mutated samples derived from AML patients, AG-120 reduced the level of intracellular 2-HG by 96% at the lowest tested dose (0.5 μM) and by 98.6% and 99.7%, respectively, at 1 and 5 μM. 5 μM AG-120 also enhanced ability of primary patient myeloblasts to form differentiated colonies in methylcellulose assays[3]. In HT1080 xenografts established in nude mice, a single oral dose of AG-120 at 50 or 150 mg/kg reduced tumor 2-HG concentration with maximum inhibition of 92.0% and 95.2%, respectively, achieved at about 12h post dose[3]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.72mL 0.34mL 0.17mL |
8.58mL 1.72mL 0.86mL |
17.15mL 3.43mL 1.72mL |
| 参考文献 |
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