Perifosine
Perifosine is an alkylphospholipid analog that exhibits anticancer chemotherapeutic and anti-inflammatory activities. Perifosine directly inhibits Akt by binding at multiple sites. In macrophages, perifosine inhibits LPS-induced increases in TNF-α and ERK activation and activates AMPK. In colorectal cancer, hepatocellular carcinoma, and multiple myeloma cells, perifosine induces apoptosis and inhibits growth; in clinical settings, perifosine enhances the anticancer activity of other chemotherapeutics.
References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/18953024
Cas No. |
157716-52-4 |
---|---|
Purity |
≥98% |
Formula |
C25H52NO4P |
Formula Wt. |
461.66 |
IUPAC Name |
(1,1-dimethylpiperidin-1-ium-4-yl) octadecyl phosphate |
Appearance |
White Crystal Powder |
Gradziel CS, Wang Y, Stec B, et al. Cytotoxic amphiphiles and phosphoinositides bind to two discrete sites on the Akt1 PH domain. Biochemistry. 2014 Jan 28;53(3):462-72. PMID: 24383815.
Shen J, Liang L, Wang C. Perifosine inhibits lipopolysaccharide (LPS)-induced tumor necrosis factor (TNF)-α production via regulation multiple signaling pathways: new implication for Kawasaki disease (KD) treatment. Biochem Biophys Res Commun. 2013 Jul 26;437(2):250-5. PMID: 23806687.
Richardson PG, Eng C, Kolesar J, et al. Perifosine, an oral, anti-cancer agent and inhibitor of the Akt pathway: mechanistic actions, pharmacodynamics, pharmacokinetics, and clinical activity. Expert Opin Drug Metab Toxicol. 2012 May;8(5):623-33. PMID: 22512706.
Fei HR, Chen G, Wang JM, et al. Perifosine induces cell cycle arrest and apoptosis in human hepatocellular carcinoma cell lines by blockade of Akt phosphorylation. Cytotechnology. 2010 Oct;62(5):449-60. PMID: 20842425.