Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 10-14 weeks | $ 767.00 | |
50 mg | 10-14 weeks | $ 997.00 | |
100 mg | 10-14 weeks | $ 1,940.00 |
Description | 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). |
Targets&IC50 | IDH1 (R132G):16.6 nM, IDH1 (R132H):15.2 nM, IDH1 (R132C):8.8 nM |
In vitro | GSK864 inhibits 2-HG production in R132C IDH1 mutant HT1080 fibrosarcoma cells (EC50: 320 nM by LCMS/MS analysis)[1]. |
In vivo | 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]. |
Molecular Weight | 558.6 |
Formula | C30H31FN6O4 |
CAS No. | 1816331-66-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (179.02 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. More
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GSK864 1816331-66-4 Others GSK-864 GSK 864 inhibitor inhibit