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    Perifosine (KRX0401)
    Perifosine (KRX0401)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0156
    CAS #: 157716-52-4Purity ≥98%

    Description: Perifosine (also known as KRX-0401) is a potent, orally bioavailable and synthetic antitumor alkylphospholipid (APL) which acts as an Akt inhibitor and a PI3K inhibitor with potential anticancer activity. As a drug candidate, it was being developed for treating a variety of cancer such as multiple myeloma and neuroblastoma. In March 2013, Aeterna Zentaris announced the discontinuing of Phase 3 clinical trial of perifosine for the treatment of relapsed and refractory multiple myeloma. Perifosine induces cell apoptosis through inhibiting the activity of Akt. Perifosine shows antitumor activity in various cell lines including NSCLC, MM, epithelial carcinoma, prostate carcinoma and leukemia cells. In H460 cells, perifosine decreased cell survival and induced apoptosis with IC50 values of 1μM and 10 μM, respectively. The treatment of perifosine was also found to induce cleavage of caspase-8, caspase-9, caspase-3 and PARP in this cell line. In MM.1S cells, perifosine induced sub-G1 phase population increase from 15% to 57% at 10 μM and induced cleavage of caspase-8, caspase-9 and PARP in a dose-dependent manner. 

    References: Mol Cancer Ther. 2007 Jul;6(7):2029-38; Blood. 2006 May 15;107(10):4053-62.

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    Molecular Weight (MW)

    461.66

    Formula

    C25H52NO4P

    CAS No.

    157716-52-4

    Storage

    -20℃ for 3 years in powder form

    -80℃ for 2 years in solvent

    Solubility (In vitro)

    DMSO: 15 mg/mL (32.5 mM)

    Water: 8 mg/mL (17.3 mM)

    Ethanol: <1 mg/mL

    Solubility (In vivo)

    30% Propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL

    Other info

    Synonym: KRX-0401; KRX 0401; KRX0401; NKA17; NSC639966; NSC 639966; NSC-639966; D 21266; D-21266

    Chemical Name: 1,1-dimethylpiperidin-1-ium-4-yl octadecyl phosphate.

    InChi Key: SZFPYBIJACMNJV-UHFFFAOYSA-N

    InChi Code: 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

    SMILES Code: O=P(OC1CC[N+](C)(C)CC1)([O-])OCCCCCCCCCCCCCCCCCC


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    In Vitro

    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: Cells (Human glioma cell lines) 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.

    Perifosine develops anti-proliferative properties with IC50 of 0.6-8.9 μM in immortalized keratinocytes (HaCaT), and head and neck squamous carcinoma cells. 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. Perifosine (10 μM) completely inhibits the phosphorylation of Akt in MM.1S cells. A recent study demonstrates Perifosine induces cell cycle arrest and apoptosis in human hepatocellular carcinoma cell lines by blockade of Akt phosphorylation.

    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. 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. Perifosine induces thrombocytosis and leukocytosis and increases myelopoiesis in murine marrow and spleen, whereas it causes apoptosis in myeloma xenografts.

    Animal model

    MM.1S MM cells are inoculated subcutaneously in the right flank of Beige-nude-xid (BNX) mice (5 to 6 weeks old).

    Formulation & Dosage

    Dissolved in 0.9% NaCl solution; 36 mg/kg; oral administration

    References

    [1] Hideshima T, et al. Blood, 2006, 107(10), 4053-4062.[2] Vyomesh Patel, et al. Cancer Res, 2002, 62(5), 1401-1409

     


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Perifosine (KRX-0401)

    Perifosine (KRX-0401)


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