Introduction
AT13148 is a novel oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity, which shows a distinct mechanism of action from other AKT inhibitors. AT13148 is currently being developed by Astex Pharmaceuticals. AT131148 was identified utilizing high-throughput X-ray crystallography and fragment-based lead discovery techniques. AT13148 caused substantial blockade of AKT, p70S6K, PKA, ROCK and SGK substrate phosphorylation and induction of apoptosis in both a concentration and time-dependent manner in cancer cells with clinically relevant genetic defects both in vitro and in vivo. AT13148 is an orally active and ATP-competitive, multi-AGC kinase inhibitor with IC50s of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively.
General Information
| Cas No. | 1056901-62-2 |
|---|---|
| Purity | >98% |
| Molecular Weight | 313.78 |
| Formula | C17H16ClN3O |
| Storage instruction | 3 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO: 1.125 g/mL at 25 °C |
.png)