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FPA 124

Names

[ CAS No. ]:
902779-59-3

[ Name ]:
FPA 124

[Synonym ]:
fpa 124

Biological Activity

[Description]:

FPA-124, a cell-permeable copper complex, is a selective Akt inhibitor with an IC50 of 0.1 μM. FPA-124 interacts with both the pleckstrin homology (PH) and the kinase domains of Akt. FPA-124 induces apoptosis[1][2].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Cancer
Signaling Pathways >> PI3K/Akt/mTOR >> Akt

[In Vitro]

FPA-124 exhibits dose-dependent growth inhibitory effects with IC50s of 7, 10, 34, and 55 μM in BT20, PC-3, COLO 357 and BxPC-3 cancer cell lines, respectively[1].

[In Vivo]

FPA-124 exhibits PKB (Akt protein) inhibitory activities and causes NF-κB inactivation in a well-established orthotopic pancreatic tumor model using COLO 357 cells[1].

[References]

[1]. Barve V, et al. Synthesis, molecular characterization, and biological activity of novel synthetic derivatives of chromen-4-one in human cancer cells. J Med Chem. 2006 Jun 29;49(13):3800-8.

[2]. Biscetti F, et al. Pioglitazone enhances collateral blood flow in ischemic hindlimb of diabetic mice through an Akt-dependent VEGF-mediated mechanism, regardless of PPARgamma stimulation. Cardiovasc Diabetol. 2009 Sep 8;8:49.

Chemical & Physical Properties

[ Molecular Formula ]:
C11H9Cl2CuN3O2S

[ Molecular Weight ]:
381.72500

[ Exact Mass ]:
379.90900

[ PSA ]:
112.71000

[ LogP ]:
3.42780

Related Compounds