Molecular Formula | C22H31N9O3 |
Molar Mass | 469.54 |
Density | 1.45±0.1 g/cm3(Predicted) |
Boling Point | 784.0±70.0 °C(Predicted) |
Solubility | DMSO: 16 mg/mL |
pKa | 14.68±0.10(Predicted) |
Storage Condition | -20℃ |
In vitro study | AZD8835 is a potent inhibitor of PI3Kα (wild type, E545K and H104R mutants) and PI3Kδ. In cells sensitive to PI3Kα inhibition and in cells sensitive to PI3Kδ inhibition, it is also a potent inhibitor of p-Akt (IC50 of 0.057 μm in human primary breast invasive ductal carcinoma BT474 cells with PIK3CA mutation and 0.049 μm in JeKo-1 B cell line), but it had little effect on those cells that were sensitive to PI3Kβ and PI3Kγ inhibition. |
In vivo study | When dosing is continued. AZD8835 has antitumor effects in a corresponding mouse model with transplanted breast tumors, with high metabolic stability and suitable physical properties when administered orally. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.13 ml | 10.649 ml | 21.297 ml |
5 mM | 0.426 ml | 2.13 ml | 4.259 ml |
10 mM | 0.213 ml | 1.065 ml | 2.13 ml |
5 mM | 0.043 ml | 0.213 ml | 0.426 ml |
Use | AZD-8835 can be used as an inhibitor in biological cell and animal experiments. |
biological activity | AZD8835 is a novel mixed inhibitor of PI3Kα and PI3Kδ with IC50 of 6.2 nM and 5.7 nM, respectively. It was also selective for PI3Kβ and PI3Kγ with IC50 of 431 nM and 90 nM, respectively. |
Target | Value |
PI3Kδ (Cell-based assay) | 5.7 nM |
PI3Kα (Cell-free assay) | 6.2 nM |
PI3Kγ (Cell-based assay) | 90 nM |
PI3Kβ (Cell-based assay) | 431 nM |