化合物 T15442 T15442

Product Introduction
Bioactivity


英文名: GSK864

描述: GSK864 is an inhibitor of isocitrate dehydrogenase 1 (IDH1) mutant. GSK864 inhibits IDH1 mutants R132C, R132H, and R132G (IC50: 8.8, 15.2, and 16.6 nM).

体外活性: GSK864 inhibits 2-HG production in R132C IDH1 mutant HT1080 fibrosarcoma cells (EC50: 320 nM by LCMS/MS analysis)[1].

体内活性: Slightly increased numbers of huCD45+ CD38+ cells in R132C or R132H IDH1 mutant engrafted mice treated with GSK864, showed from analysis of BM cells for expression of markers of early differentiation. Significant concentrations of GSK864 are maintained in peripheral blood samples of mice for up to 24 hours, following intraperitoneal (IP) administration in CD-1 mice[1].

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

溶解度: DMSO : 100 mg/mL (179.02 mM)


关键字: GSK-864 | GSK 864 | GSK864

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途