CAS No. 958852-01-2
| IUPAC Name | (5Z)-5-[(4-pyridin-4-ylquinolin-6-yl)methylidene]-1,3-thiazolidine-2,4-dione | |
|---|---|---|
| CAS Number | 958852-01-2 | |
| Molecular Formula |
C18H11N3O2S |
|
| Molecular Weight (MW) | 333.36 | |
| SMILES | C1=CC2=NC=CC(=C2C=C1C=C3C(=O)NC(=O)S3)C4=CC=NC=C4 | |
| InChIKey | QDITZBLZQQZVEE-YBEGLDIGSA-N |
GSK1059615 is a potent, reversible dual inhibitor of PI3Kα (IC50 0.4 nM), PI3Kβ (IC50 0.6 nM), PI3Kδ (IC50 2 nM), PI3Kγ (IC50 5 nM), and mTOR (IC50 12 nM). By blocking the PI3K/AKT/mTOR pathway, GSK1059615 inhibits cellular proliferation and induces G1 cell cycle arrest and apoptosis. In xenograft mouse models, GSK1059615 demonstrates robust antitumor activity, causing complete tumor growth inhibition and regression accompanied by increased plasma insulin levels.
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Concentration
Volume
Mass
|
|---|
| Solvent | Solubility & Note |
|---|---|
| DMSO |
2 mg/mL
(5.99 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.) |
| Water | Insoluble |
| Ethanol | Insoluble |
- Preheat media/saline to 37°C.
- Mix rapidly (pipette/vortex) upon addition.
- For complex mixes, always add the aqueous phase last.
- Re-dissolve minor precipitates with a 37°C water bath and sonication (≤30 min).
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