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A-674563 is a potent selective Akt1 (Protein Kinase B) inhibitor. A-674563 also shows inhibitory activity against PKA and CDK2 with IC50 values of 16nM and 46nM respectively. 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 | 358.44 |
| Formula | C22H22N4O |
| CAS Number | 552325-73-2 |
| Solubility (25°C) | DMSO 60 mg/mL Water 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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| FPA-124
FPA-124, a cell-permeable copper complex, is a selective Akt inhibitor with an IC50 of 0.1 μM. |
| SPOP-IN-1
SPOP-IN-1 is a selective SPOP E3 ubiquitin ligase inhibitor. |
| 10-DEBC hydrochloride
10-DEBC hydrochloride is a selective Akt inhibitor, with an IC50 of 1.28 μM. |
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