Date published: 2025-9-13

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A-674563 (CAS 552325-73-2)

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Alternate Names:
(2s)-1-{[5-(3-Methyl-1h-Indazol-5-Yl)pyridin-3-Yl]oxy}-3-Phenylpropan-2-Amine
Application:
A-674563 is a selective Akt1, PKA, and CDK2 inhibitor
CAS Number:
552325-73-2
Molecular Weight:
358.44
Molecular Formula:
C22H22N4O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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A-674563 is a potent selective protein kinase B/Akt inhibitor (IC50 = 14 nM). A-674563 also shows inhibitory activity against PKA and CDK2 (IC50′s: PKA = 16 nM; CDK2 = 46 nM). A-674563 has been shown to have a significant effect on depolarization of purkinje fiber in an in vitro assay, and severe CV toxicity (e.g. hypotension) in vivo. The X-ray structure of A-674563 bound to protein kinase A, which exhibts 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 (EC50: 0.4 μM). When given in combination, A-674563 enhanced the efficacy of paclitaxel (Taxol, sc-201439) in a PC-3 xenograft model.


A-674563 (CAS 552325-73-2) References

  1. Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo.  |  Luo, Y., et al. 2005. Mol Cancer Ther. 4: 977-86. PMID: 15956255
  2. Concurrent targeting Akt and sphingosine kinase 1 by A-674563 in acute myeloid leukemia cells.  |  Xu, L., et al. 2016. Biochem Biophys Res Commun. 472: 662-8. PMID: 26920060
  3. Pre-clinical assessment of A-674563 as an anti-melanoma agent.  |  Zou, Y., et al. 2016. Biochem Biophys Res Commun. 477: 1-8. PMID: 26970307
  4. A-674563 increases chondrocyte marker expression in cultured chondrocytes by inhibiting Sox9 degradation.  |  Kobayashi, T., et al. 2018. Biochem Biophys Res Commun. 495: 1468-1475. PMID: 29196261
  5. A-674563, a putative AKT1 inhibitor that also suppresses CDK2 activity, inhibits human NSCLC cell growth more effectively than the pan-AKT inhibitor, MK-2206.  |  Chorner, PM. and Moorehead, RA. 2018. PLoS One. 13: e0193344. PMID: 29470540
  6. Mesenchymal Stem Cells Improve Glycometabolism and Liver Regeneration in the Treatment of Post-hepatectomy Liver Failure.  |  Ding, HR., et al. 2019. Front Physiol. 10: 412. PMID: 31024348
  7. Integration of mechanical conditioning into a high throughput contractility assay for cardiac safety assessment.  |  Goßmann, M., et al. 2020. J Pharmacol Toxicol Methods. 105: 106892. PMID: 32629160
  8. Resveratrol Targets AKT1 to Inhibit Inflammasome Activation in Cardiomyocytes Under Acute Sympathetic Stress.  |  Wang, R., et al. 2022. Front Pharmacol. 13: 818127. PMID: 35250567
  9. Combined immune and DDR pathway classifier: A novel pathway-based classification aimed at tailoring personalized therapies for acute myeloid leukemia patients.  |  Huang, Y., et al. 2023. Comput Biol Med. 162: 107093. PMID: 37269679
  10. Potential role of Akt in the regulation of fibroblast growth factor 21 by berberine.  |  Hirai, T., et al. 2024. J Nat Med. 78: 169-179. PMID: 37951850

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

A-674563, 2 mg

sc-364393
2 mg
$232.00

A-674563, 5 mg

sc-364393A
5 mg
$413.00