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GSK864

  Cat. No.:  DC32537   Featured
Chemical Structure
1816331-66-4
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More than 5000 active chemicals with high quality for research!
Field of application
GSK864 is a potent and selective inhibitor of mutant IDH1. GSK864 inhibits IDH1 mutants R132C/R132H/R132G with IC50 values of 9/15/17 nM, respectively, and is moderately selective over wild-type IDH1 and IDH2 mutants/wild-type. Treatment of R132C IDH1 mutant HT-1080 cells for 24 hours with GSK864 results in a dose-dependent reduction of 2-hydroxyglutarate (2-HG), which is not observed with GSK990, a structurally similar compound which is inactive as an IDH1 inhibitor. GSK864 has been shown to be selective in vitro for IDH1 over other classes of proteins (7TMs, ion channels, kinases) and chemoproteomic studies with GSK321, an analog of GSK864, confirm selective binding of IDH1 by this chemical series. GSK864 has a pharmacokinetic profile suitable for in vivo studies.
Chemicals PropertiesBiological activity Related products COA MSDS Datasheet
Cas No.: 1816331-66-4
Chemical Name: GSK864
Synonyms: GSK864;GSK-864
SMILES: FC1=CC=C(CN2C3C(CN(CC=3C(C(=O)NC3C=C(C)C(OC)=C(C)C=3)=N2)C(=O)C2NC=CC=2)(C)C(=O)N)C=C1
Formula: C30H31FN6O4
M.Wt: 558.603349924088
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: 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.
Target: IC50: 8.8 nM (IDH1 mutants R132C), 15.2 nM (IDH1 mutants R132H), 16.6 nM (IDH1 mutants R132G)[1]
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[1].
In Vitro: GSK864 inhibits 2-HG production in R132C IDH1 mutant HT1080 fibrosarcoma cells with an EC50 of 320 nM by LCMS/MS analysis[1].
Animal Administration: Mice: Mice receive GSK864 (213 mg/kg, 10 mL/kg) via intraperitoneal (ip) administration. IP formulation is PG:DMSO:PEG400:H2O (16.7:3.3:40:40). Serial blood samples (~0.030 mL) are collected via the femoral artery catheter at 15, 30, 45, 60, 120, 180 min following administration[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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