Chemical Name
Piperidinium, 4-[[hydroxy(octadecyloxy)phosphinyl]oxy]-1,1-dimethyl-, inner salt
In vitro
Perifosine (D-21266, KRX-0401) is an analogue of miltefosine. Perifosine, a bioavailable ALK (Alkylphospholipids)showed antiproliferative properties on the cell cycle kinetics of immortalized keratinocytes (HaCaT) as well as head and neck squamous carcinoma cells with an IC50 of 0.6-8.9 uM. Perifosine induced both G(1)-S and G(2)-M cell cycle arrest at the concentration of 20 uM, together with p21(WAF1) expression in both p53 wild-type and p53(-/-) clones.Perifosine blocks cell cycle progression of head and neck squamous carcinoma cells at G(1)-S and G(2)-M by inducing p21(WAF1), irrespective of p53 function. Perifosine causes dose-dependent inhibition of protein kinase B/Akt phosphorylation and thus activation at concentrations causing growth inhibition of PC-3 prostate carcinoma cells. perifosine decreases the plasma membrane localization of Akt, and this is substantially relieved by MYR-Akt along with relief of downstream drug effect on induction of p21(WAF1/CIP1). Perifosine does not directly affect phosphoinositide 3-kinase (PI3K), phosphoinositide-dependent kinase 1, or Akt activity at concentrations inhibiting Akt phosphorylation and membrane localization.
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