| Molecular Formula | C21H22N6O3 |
| Molar Mass | 406.44 |
| Density | 1.59 |
| Melting Point | >149°C (subl.) |
| Solubility | DMSO (Slightly) |
| Appearance | Solid |
| Color | Pale Beige to Light Beige |
| pKa | 4.44±0.10(Predicted) |
| Storage Condition | Hygroscopic, -20°C Freezer, Under inert atmosphere |
| In vitro study | OSI-027 showed selective and ATP competitive inhibitory activity against mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM, respectively. In addition, the mTOR signal of phospho-4e-bp was inhibited by OSI-027, and the IC50 in the cell assay was 1 μm. OSI-027 exhibited dose-dependent antiproliferative activity against several acute leukemia cell lines derived from bone marrow/megakaryocytes, including U937,KG-1,KBM-3B,ML-1,HL-60, and MEG-01 cells. A recent study showed that OSI-027 inhibition of mTORC1/2 effectively inhibited Akt (S473) phosphorylation and cell proliferation in breast cancer cells. |
| In vivo study | In GEO colorectal xenografts, OSI-027 (65 mg/kg) inhibited phosphorylation of mTORC1 and mTORC2 effectors, including 4E-BP1,Akt, and S6. In addition, OSI-027 inhibited both mTORC1 and mTORC2, and the inhibition of mTORC1 was more effective than that of rapamycin. |
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.46 ml | 12.302 ml | 24.603 ml |
| 5 mM | 0.492 ml | 2.46 ml | 4.921 ml |
| 10 mM | 0.246 ml | 1.23 ml | 2.46 ml |
| 5 mM | 0.049 ml | 0.246 ml | 0.492 ml |