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A-674563 hydrochloride is a potent and selective Akt1 inhibitor with Ki of 11 nM. A-674563 has a significant effect on depolarization of purkinje fiber in an in vitro assay, and severe CV toxicity (e.g. hypotension) in vivo. A-674563 induced Akt blockade results in decreased STS cell downstream target phosphorylation and tumor cell growth inhibiton. A-674563 (0-30 µM) reduces the phosphorylation of GSK3α/β, TSC2, mTOR, and ribosomal protein S6 in a dose-dependent fashion in MiaPaCa-2 cells in vitro. Furthermore, A-674563 inhibits hERG ion channels in vitro and causes acute hypotension in vivo. A674563-treated (20 mg/kg/bid, p.o.) mice exhibits slower tumor growth and more than 50% decrease in the tumor volume at the termination of the study compared with that in control group.
| Molecular Weight | 394.9 |
| Formula | C22H23ClN4O |
| CAS Number | 2070009-66-2 |
| Solubility (25°C) | Water 60 mg/mL DMSO 50 mg/mL |
| Storage | 2-8°C, sealed |
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