| 应用 |
A selective Akt1, PKA, and CDK2 inhibitor |
| 产品介绍 |
A-674563是Akt1抑制剂，IC50为14 nM，还能抑制PKA和CDK2，IC50分别为16和46 nM。 |
| 备注 |
A-674563 is an Akt1 inhibitor with Ki of 11 nM, modest potent to PKA and >30-fold selective for Akt1 over PKC. |
| 生化机理 |
A-674563 is achieved from A-443654 by replacing the indole with a phenyl moiety and getting oral activity. A-674563 slows proliferation of tumor cells with EC50 of 0.4 μM. A-674563 does not inhibit Akt phosphorylation per se, but blocks the phosphorylation of Akt downstream targets in a dose-dependent manner. A-674563 induced Akt blockade results in decreased STS cell downstream target phosphorylation and tumor cell growth inhibiton. A-674563 induces G2 cell cycle arrest and apoptosis in STS cells. |
| 别名 |
A 674563; A674563;(alphas)-alpha-(((5-(3-methyl-1h-indazol-5-yl)-3-pyridinyl)oxy)methyl)benzeneethanamine;(2s)-1-{[5-(3-Methyl-1h-Indazol-5-Yl)pyridin-3-Yl]oxy}-3-Phenylpropan-2-Amine;A 674563; A674563; (alphaS)-alpha-(((5-(3-甲基-1H-吲唑-5-基)-3-吡啶基)氧)甲基)苯乙胺; |
![ACTH [1-17]](http://img.antpedia.com/cbook/attachments/product/6751/1_a118750-1mg.gif!w456x328.gif)