Product Introduction
Bioactivity


英文名: Mutant IDH1-IN-6

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.

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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: Mutant IDH1 IN 6 | Mutant IDH-1-IN-6 | Mutant IDH1IN6