GSK864 |
| カタログ番号GC17809 |
GSK864 は、イソクエン酸デヒドロゲナーゼ 1 (IDH1) 変異阻害剤です。 IDH1 変異体 R132C、R132H、および R132G を 8.8、15.2、および 16.6 nM の IC50 値で阻害します。
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Cas No.: 1816331-66-4
Sample solution is provided at 25 µL, 10mM.
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GSK864 is an isocitrate dehydrogenase 1 (IDH1) mutant inhibitor; inhibits IDH1 mutants R132C, R132H, and R132G with IC50 values of 8.8, 15.2 and 16.6 nM.
GSK864 inhibits 2-HG production in R132C IDH1 mutant HT1080 fibrosarcoma cells with an EC50 of 320 nM by LCMS/MS analysis[1].
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[1].
References:
[1]. Okoye-Okafor UC, et al. New IDH1 mutant inhibitors for treatment of acute myeloid leukemia. Nat Chem Biol. 2015 Nov;11(11):878-86.
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