Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Mutant IDH1-IN-6 is an orally active compound that effectively inhibits mutant isocitrate dehydrogenase (IDH) enzymes. It demonstrates potency and selectivity, with IC50 values of 6.27, 3.71, 36.9, and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q, and IDH2 R172K mutants, respectively. Notably, Mutant IDH1-IN-6 exhibits lower activity in inhibiting wild-type IDH enzymes.
产品描述 | Mutant IDH1-IN-6 is an orally active compound that effectively inhibits mutant isocitrate dehydrogenase (IDH) enzymes. It demonstrates potency and selectivity, with IC50 values of 6.27, 3.71, 36.9, and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q, and IDH2 R172K mutants, respectively. Notably, Mutant IDH1-IN-6 exhibits lower activity in inhibiting wild-type IDH enzymes. |
靶点活性 | IDH2 (R172K):11.5 nM (IC50), IDH1 (R132C):3.71 nM (IC50), IDH2 (R140Q):36.9 nM (IC50), IDH1 (R132H):6.27 nM (IC50), IDH2 (WT):884 nM (IC50), IDH1 (WT):105 nM (IC50) |
体外活性 | Mutant IDH1-IN-6 (example 2) inhibits production of 2-hydroxyglutarate in HT1080 cells with an IC50 of 1.28 nM, indicating the inhibition of mutant IDHl R132C in cells. aKG, a metabolite generated by wild-type IDHl is not affected by Mutant IDH1-IN-6, indicating Mutant IDH1-IN-6 is selective for mutant IDHl over wild type IDHl in cells[1]. |
体内活性 | Mutant IDH1-IN-6 (Example 2; 0-32 mg/kg; oral gavage; twice daily; for 3 days) treatment inhibitis of 2-hydroxyglutarate in a dose-dependent manner in IDHl mutant xenograft mice[1]. Animal Model: Athymic nude mice (20-22 g) injected with TB08 cells[1]Dosage: 1 mg/kg, 2 mg/kg, 4 mg/kg, 8 mg/kg, 16 mg/kg, 32 mg/kg Administration: Oral gavage; twice daily; for 3 days Result: Inhibitied of 2-hydroxyglutarate in IDHl mutant xenograft mice. |
别名 | Mutant IDH1-IN-6 |
分子量 | 504.635 |
分子式 | C28H36N6O3 |
CAS No. | 2230263-60-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Mutant IDH1-IN-6 2230263-60-0 Mutant IDH1 IN 6 Mutant IDH-1-IN-6 Mutant IDH1IN6 Inhibitor inhibitor inhibit