GSK864,1816331-66-4

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GSK864

CAS No. : 1816331-66-4

MCE 国际站：GSK864

产品活性：GSK864是异柠檬酸脱氢酶1 (IDH1) 突变体抑制剂; 抑制IDH1突变体R132C，R132H和R132G的IC₅₀值分别为8.8，15.2和16.6 nM。

研究领域：Metabolic Enzyme/Protease

作用靶点：Isocitrate Dehydrogenase (IDH)

In Vitro: GSK864 inhibits 2-HG production in R132C IDH1 mutant HT1080 fibrosarcoma cells with an EC₅₀ of 320 nM by LCMS/MS analysis.

In Vivo: Following intraperitoneal (IP) administration in CD-1 mice, significant concentrations of GSK864 are maintained in peripheral blood samples of mice for up to 24 hours. Analysis of BM cells for expression of markers of early differentiation reveals slightly increased numbers of huCD45⁺ CD38⁺ cells in R132C or R132H IDH1 mutant engrafted mice treated with GSK864.

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