AZD8835 is a potent and selective inhibitor of PI3Kalpha and PI3Kdelata with excellent general kinase selectivity. AZD8835 displayed low metabolic turnover and suitable physical properties for oral administration. At the enzyme level, AZD8835 is a potent mixed inhibitor of PI3Kα (IC50 0.0062 μM) and PI3Kδ (IC50 0.0057 μM), with selectivity against PI3Kβ (IC50 0.431 μM) and PI3Kγ (IC50 0.090 μM). In vivo, AZD8835 showed pharmacodynamic modulation of AKT phosphorylation and near complete inhibition of tumour growth (93% tumour growth inhibition) in a murine H1047R PI3Kalpha mutated SKOV-3 xenograft tumour model after chronic oral administration at 25 mg/kg b.i.d. AZD8835, is currently in phase I clinical trials.
MedKoo Cat#: 206479
Name: AZD8835
CAS#: 1620576-64-8
Chemical Formula: C22H31N9O3
Exact Mass: 469.2550
Molecular Weight: 469.55
Elemental Analysis: C, 56.28; H, 6.65; N, 26.85; O, 10.22
| Solvent | mg/mL | mM | comments | |
|---|---|---|---|---|
| Solubility | ||||
| DMSO | 43.0 | 91.58 | ||
| DMSO:PBS (pH 7.2) (1:1) | 0.5 | 1.06 | ||
| DMF | 16.0 | 34.08 | ||
| Ethanol | 2.0 | 4.26 |
The following data is based on the product molecular weight 469.55 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
