AZD8186
AZD8186
CAS: 1627494-13-6
Molecular Formula: C24H25F2N3O4
AZD8186 - Names and Identifiers
AZD8186 - Physico-chemical Properties
| Molecular Formula | C24H25F2N3O4 |
| Molar Mass | 457.47 |
| Density | 1.351±0.06 g/cm3(Predicted) |
| Melting Point | 226-227°C |
| Boling Point | 645.2±55.0 °C(Predicted) |
| Solubility | DMSO: ≥ 35 mg/mL |
| Appearance | Solid |
| Color | White to Off-White |
| pKa | 2.56±0.50(Predicted) |
| Storage Condition | -20°C Freezer |
| In vitro study | In MDA-MB-468 cells sensitive to PI3Kβ inhibition and Jeko B cells sensitive to PI3Kδ inhibition, AZD8186 effectively inhibited p-Akt with an IC50 of 3 nM and 4 nM, respectively. AZD8186 showed the highest growth inhibitory activity in most PTEN-deleted cell lines with GI50 <1 μm. |
| In vivo study | In nude mice loaded with PTEN-deleted PC3 prostate tumor xenografts, AZD8186 (100 mg/kg, p.o.) strongly inhibited Akt phosphorylation levels and caused significant tumor growth inhibition. AZD8186 (60 mg/kg, p.o.) completely inhibited tumor growth when used in combination with ABT. AZD8186 (50 mg/kg, p.o.) also inhibited tumor growth in the mouse PTEN-deleted TNBC model, HCC70 and MDA-MB-468, and in the prostate model, hid28. The combination of AZD8186 with chemocastration resulted in durable tumor regression that persisted after cessation of treatment. |
AZD8186 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.186 ml | 10.93 ml | 21.859 ml |
| 5 mM | 0.437 ml | 2.186 ml | 4.372 ml |
| 10 mM | 0.219 ml | 1.093 ml | 2.186 ml |
| 5 mM | 0.044 ml | 0.219 ml | 0.437 ml |
Last Update：2024-01-02 23:10:35
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