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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 | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $68 | - | In Stock | |
| 5 mg | $163 | - | In Stock | |
| 10 mg | $263 | - | In Stock | |
| 25 mg | $423 | - | In Stock | |
| 50 mg | $595 | - | 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 | 2-HG:320 nM (EC50), IDH1 (R132G):16.6 nM, IDH1 (R132C):8.8 nM, IDH1 (R132H):15.2 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]. |
| Synonyms | 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) |
| Color | White |
| Appearance | Solid |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 100 mg/mL (179.02 mM), Sonication is recommended. H2O: < 1 mg/mL (Insoluble) | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (7.16 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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