Stereochemistry | ACHIRAL |
Molecular Formula | C25H52NO4P |
Molecular Weight | 461.6584 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CCCCCCCCCCCCCCCCCCOP([O-])(=O)OC1CC[N+](C)(C)CC1
InChI
InChIKey=SZFPYBIJACMNJV-UHFFFAOYSA-N
InChI=1S/C25H52NO4P/c1-4-5-6-7-8-9-10-11-12-13-14-15-16-17-18-19-24-29-31(27,28)30-25-20-22-26(2,3)23-21-25/h25H,4-24H2,1-3H3
Perifosine is an orally active alkyl-phosphocholine compound with potential antineoplastic activity. Perifosine is an Akt inhibitor, which targets the pleckstrin homology domain of Akt, thereby preventing its translocation to the plasma membrane. Perifosine exerts Akt-dependent and Akt-independent effects, and although many preclinical studies have documented Akt inhibition by perifosine, clinical validation of these findings is lacking. Perifosine is in phase II and III clinical trials for the treatment of neuroblastoma, glioblastoma multiforme and other solid tumors.
CNS Activity
Originator
Approval Year
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Drug as victim
Sourcing
PubMed
Patents
Sample Use Guides
Growth inhibitoy activities of Perifosine against selected human cell lines appeared to be slightly more potent than activity of miltefosine. Thus, IC50s of Perifosine for melanoma cell lines M14 and SK-NEL-28 were 2.6 uM/ml and 19.9 uM/ml respectively; for CNS cell line SF-295 – 3.1 uM/ml; for prostate cell line PC-3 – 1.5 uM/ml; for Colon cell lines KM12, HT29, HCT-116 – 0.2 uM/ml, 4.0 uM/ml and 10.2 uM/ml respectively.