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GSK864 is an IDH1 mutant inhibitor that inhibits IDH1 mutants R132C, R132H, and R132G, and is used in the study of cardiovascular and oncology diseases.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $68 | In Stock | |
5 mg | $163 | In Stock | |
10 mg | $293 | In Stock | |
25 mg | $579 | In Stock | |
50 mg | $928 | In Stock | |
100 mg | $1,480 | In Stock | |
1 mL x 10 mM (in DMSO) | $197 | In Stock |
Description | GSK864 is an IDH1 mutant inhibitor that inhibits IDH1 mutants R132C, R132H, and R132G, and is used in the study of cardiovascular and oncology diseases. |
Targets&IC50 | IDH1 (R132H):15.2 nM, 2-HG:320 nM (EC50), IDH1 (R132C):8.8 nM, IDH1 (R132G):16.6 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 | In mice with R132C or R132H IDH1 mutant transplants treated with GSK864 (IP), the number of huCD45+ CD38+ cells showed a slight increase [1]. |
Alias | GSK-864, GSK 864 |
Molecular Weight | 558.6 |
Formula | C30H31FN6O4 |
Cas No. | 1816331-66-4 |
Smiles | COc1c(C)cc(NC(=O)c2nn(Cc3ccc(F)cc3)c3c2CN(C[C@]3(C)C(N)=O)C(=O)c2ccc[nH]2)cc1C |
Relative Density. | 1.37 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (179.02 mM), Sonication is recommended. H2O: < 1 mg/mL (Insoluble) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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