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. |