Molecular Formula | C21H25ClN6O2 |
Molar Mass | 428.92 |
Density | 1.381 |
Melting Point | 161-164°C |
Solubility | DMSO (Slightly), Methanol (Slightly) |
Appearance | Solid |
Color | Off-White to Pale Beige |
pKa | 13.93±0.50(Predicted) |
Storage Condition | Refrigerator |
In vitro study | AZD5363 is a potent inhibitor of Akt, inhibiting Akt1, Akt2 and Akt3 with IC50 of 3 nM, 8 nM and 8 nM, respectively. The activation of PIK3CA mutation, the loss or inactivation of the tumor suppressor gene PTEN, or the amplification of HER2 all have a significant relationship with AZD5363. Furthermore, a correlation between the RAS mutational status of the cell lines and the anti-azd5363 can also be seen. AZD5363 inhibited phosphorylation of AKT substrates in cells with a titer of about 0.3~0.8 μm. AZD5363 inhibited cell proliferation in 41 of 182 solid and hematologic tumor cell lines with a titer of <3 μm. |
In vivo study | AZD5363 was orally administered to nude mice at a dose of 100,300 mg/kg to reduce the phosphorylation of PRAS40, GSK3β, and S6 in the transplanted tumor of BT474c in a dose-and time-dependent manner, it also reversibly increases blood glucose concentration and reduces 2 [ |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.331 ml | 11.657 ml | 23.314 ml |
5 mM | 0.466 ml | 2.331 ml | 4.663 ml |
10 mM | 0.233 ml | 1.166 ml | 2.331 ml |
5 mM | 0.047 ml | 0.233 ml | 0.466 ml |