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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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| AT7867
AT7867 is a potent and oral inhibitor of AKT and p70 S6 kinase with an IC50 of 17 nM. |
| GSK690693
GSK690693 is a potent Akt inhibitor (Akt1 IC50 = 2 nM, Akt2 IC50 = 13 nM, Akt3 IC50 = 9 nM) which also inhibited the phosphorylation of the downstream target GSK3b in cells. |
| Perifosine
Perifosine is an orally active Akt inhibitor, the antiproliferative properties of Perifosine with an IC50 of 0.6–8.9 µM. |
| MK-2206 2HCl
MK-2206 is a novel allosteric inhibitor of Akt with IC50 values of 8 nM, 12 nM and 65 nM for Akt1, Akt2 and Akt3, respectively. |
| Ipatasertib
Ipatasertib (GDC-0068, RG7440) is a potent and selective, ATP-competitive Akt inhibitor with IC50 values of 5 to 18 nM. |
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