Molecular Formula | C15H15N7O
|
Molar Mass | 309.33 |
Density | 1.64 |
Melting Point | 270-272°C (dec.) |
Boling Point | 598.8±60.0 °C(Predicted) |
Solubility | Soluble in DMSO (up to 25 mg/ml) |
Appearance | solid |
Color | Off-white |
pKa | 3.77±0.30(Predicted) |
Storage Condition | -20°C |
Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
In vitro study | The INK 128 exhibited inhibitory activity against mTOR enzymes and was more than 100-fold selective for PI3K kinase. As a TORC1/2 inhibitor, INK 128 inhibits the phosphorylation of the downstream substrates of TORC1, S6 and 4EBP1. In addition, the INK 128 also showed potent inhibitory effects on cell lines resistant to rapamycin and pan-PI3K inhibitors. |
In vivo study | In a ZR-75-1 breast cancer xenograft model, treatment with INK 128(0.3 mg/kg/day) demonstrated tumor growth inhibition. Daily oral administration of INK 128 inhibits angiogenesis and tumor growth in a variety of transplant models. |