A-674563 is a potent and selective PKB/Akt inhibitor with an IC50 of 14 nM. It binds to ATP-binding site of Akt and reduces the phosphorylation of Akt's downstream targets (GSK3α/β, FOXO3, TSC2, mTOR and S6, etc.). A-674563 also inhibits activity of PKA and CDK2 with IC50 of 16 and 46 nM, respectively. A-674563 inhibits proliferation of tumor cells with IC50 of 0.4 µM1.
In STS cells, A-674563 induces Akt pathway blockade that decreases downstream target phosphorylation, and induces G2 cell cycle arrest and apoptosis. In vivo, A-674563 reduces STS xenograft growth2. When given in combination, A-674563 enhanced the efficacy of paclitaxel in a PC-3 xenograft model1.
Technical information:
| Chemical Formula: | C22H22N4O | |
| CAS #: | 552325-73-2 | |
| Molecular Weight: | 358.44 | |
| Purity: | >98% | |
| Appearance: | White solid | |
| Chemical Name: | (2S)-1-(5-(3-methyl-1H-indazol-5-yl)pyridin-3-yloxy)-3-phenylpropan-2-amine | |
| Solubility: | Up to 100 mM in DMSO |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Luo Y, et al. Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo. Mol Cancer Ther. 2005. 4(6):977-86. PMID: 15956255 |
| 2. | Zhu QS, et al. Soft tissue sarcoma cells are highly sensitive to AKT blockade: a role for p53-independent up-regulation of GADD45 alpha. Cancer Res. 2008. 68(8):2895-903. PMID: 18413758 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
