Research Area
Product Type
United States ( Change Country )
A-674563 Chemical Structure
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Biological Activity
A-674563 is a potent selective protein kinase B/Akt inhibitor with an IC50 of 14 nM. A-674563 also shows inhibitory activity against PKA and CDK2 with IC50 of 16 and 46 nM, respectively. While promising efficacy was observed in vivo, A-674563 indicated significantly effects on depolarization of purkinje fiber in an in vitro assay and severe CV toxicity (e.g. hypotension) in vivo. An X-ray structure of A-674563 bound to protein kinase A, which has 80% homology with Akt in the kinase domain, suggested the phenyl group is not tightly bound in the ligand-protein complex. The Akt inhibitor A-674563 displayed proliferation of tumor cells with an EC50 of 0.4 μM. When given in combination, A-674563 enhanced the efficacy of paclitaxel in a PC-3 xenograft model.[1][2]
References on A-674563
- [1] Mol Cancer Ther. 2005 Jun;4(6):977-86
- [2] March 2005;
Chemical Information
| Molecular Weight (WM): | 358.44 |
|---|---|
| Formula: | C22H22N4O |
| CAS No.: | 552325-73-2 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | DMSO ≥72mg/mL |
| Water ≥72mg/mL | |
| Ethanol ≥12mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
Research Area
Cell Cycle / Checkpoint >> CDK >> CDK Inhibitors
Others >> PKA >> PKA Inhibitors
PI3K / mTOR / AKT >> AKT >> AKT Inhibitors
Others >> PKA >> PKA Inhibitors
PI3K / mTOR / AKT >> AKT >> AKT Inhibitors
Notes:
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