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Perifosine

Catalog No. S1037 Name Selleck Chemicals
CAS Number 157716-52-4 Website http://www.selleckchem.com
M. F. C25H52NO4P- Telephone (877) 796-6397
M. W. 461.658441 Fax (832) 582-8590
Purity Email sales@selleckchem.com
Storage -20°C Chembase ID: 72598

SYNONYMS

IUPAC name
{[(1,1-dimethylpiperidin-1-ium-4-yl)oxy](octadecyloxy)phosphoryl}-$l^{3}-oxidanediide
IUPAC Traditional name
[(1,1-dimethylpiperidin-1-ium-4-yl)oxy(octadecyloxy)phosphoryl]-$l^{3}-oxidanediide
Synonyms
NSC 639966
KRX-0401

DATABASE IDS

CAS Number 157716-52-4

PROPERTIES

Target Akt
Target PI3K
Salt Data Free Base
Solubility H2O
Storage Condition -20°C

DETAILS

Description (English)
Biological Activity
Description Perifosine (KRX-0401) is a novel Akt inhibitor with IC50 of 4.7 μM.
Targets AKT
IC50 4.7 μM [1]
In Vitro Perifosine strongly reduces phosphorylation levels of Akt and extracellular signal-regulated kinase (Erk) 1/2, induces cell cycle arrest in G1 and G2, and causes dose-dependent growth inhibition of mouse glial progenitors. [2] Perifosine develops anti-proliferative properties with an IC50 of 0.6-8.9 μM in immortalized keratinocytes (HaCaT), and head and neck squamous carcinoma cells. [1] Perifosine (10 μM) completely inhibits the phosphorylation of Akt in MM.1S cells in a time-dependent fashion.[3] A recent study demonstrates Perifosine induces cell cycle arrest and apoptosis in human hepatocellular carcinoma cell lines by blockade of Akt phosphorylation. [4]
In Vivo Perifosine combining with temozolomide reduces tumor proliferation (a PDGF-driven gliomagenesis) in vivo. The results indicate that Perifosine is an effective drug in gliomas in which Akt and Ras-Erk 1/2 pathways are frequently activated, and may be new candidate for glima treatment in the clinic. [2] Both oral daily and weekly administration of Perifosine significantly reduce human MM tumor growth and increase survival, compared with control animals treated with PBS vehicle only. [3] Perifosine induced thrombocytosis and leukocytosis and increased myelopoiesis in murine marrow and spleen, whereas it causes apoptosis in myeloma xenografts. [5]
Clinical Trials Perifosine is undergoing its Phase III clinical trials for the treatment of refractory multiple myeloma, in combination with a Placebo, and is in Phase II trials for several other cancers.
Features
Protocol
Kinase Assay [3]
Akt kinase assay MM.1S cells are cultured in the presence or absence of perifosine (5 μM, 6 hours) and then stimulated with IL-6 (20 ng/mL, 10 minutes). In vitro akt kinase assay is then carried out using the Akt Kinase Assay Kit.
Cell Assay [2]
Cell Lines Human glioma cell lines
Concentrations 0, 15, 30 and 45 μM
Incubation Time 48 hours
Methods Cells are incubated in the medium with 10% FCS for 48 hours with indicated concentration of Periosine. Cell viability is determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. (Cell Proliferation Kit I; Roche). The absorbance at 590 nm is recorded using the 96-well plate reader.
Animal Study [3]
Animal Models MM.1S MM cells are inoculated subcutaneously in the right flank of Beige-nude-xid (BNX) mice (5 to 6 weeks old).
Formulation 0.9% NaCl solution
Doses 250 mg/kg/wk or 36 mg/kg/d
Administration Oral gavage
References
[1] Vyomesh Patel, et al. Cancer Res, 2002, 62(5), 1401-1409
[2] Momota H, et al. Cancer Res, 2005, 65(16), 7429-7435.
[3] Hideshima T, et al. Blood, 2006, 107(10), 4053-4062.
[4] Fei HR, et al. Cytotechnology, 2010, 62(5), 449-460
[5] Catley L, et al. Exp Hematol, 2007, 32(7), 1038-1046