| Description | AMG319 is a potent and selective PI3Kδ inhibitor with IC50 of 18 nM, >47-fold selectivity over other PI3Ks. Phase 2. |
| In vitro | AMG319以8.6 nM的IC50抑制抗IgM/CD40L诱导的B细胞增殖，并以1.5 nM的IC50降低pAkt水平。AMG319还抑制HWB中由抗IgD诱导的CD-69表达。[1] |
| In vivo | 在雌性Lewis大鼠中，AMG319（3 mg/kg，口服）通过88%抑制了KLH诱导的炎症反应。在转基因(IgMm)小鼠中，AMG319（口服）抑制体内pAKT，IC50为1.9 nM。[1] |
| Target activity | PI3Kδ:18 nM |
| molecular weight | 385.4 |
| Molecular formula | C21H16FN7 |
| CAS | 1608125-21-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 71 mg/mL (184.2 mM) Ethanol: 71 mg/mL (184.2 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) |
| References | 1. Cushing TD, et al. J Med Chem. 2015, 58(1), 480-511. |