2. PI3K/Akt/mTOR Autophagy Apoptosis
  3. Akt Autophagy Apoptosis
  4. Perifosine

Perifosine  (Synonyms: KRX-0401; NSC 639966; D21266)

Cat. No.: HY-50909 Purity: ≥98.0%
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Perifosine is an oral Akt inhibitor which inhibits proliferation of different tumor cell lines with IC50s of 0.6-8.9 μM.

For research use only. We do not sell to patients.

Perifosine Chemical Structure

Perifosine Chemical Structure

CAS No. : 157716-52-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
 USD 87 In-stock
Solution
10 mM * 1 mL in Water USD 87 In-stock
Solid
1 mg USD 32 In-stock
5 mg USD 79 In-stock
10 mg USD 106 In-stock
50 mg USD 363 In-stock
100 mg USD 581 In-stock
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Based on 14 publication(s) in Google Scholar

Perifosine Related Antibodies

Top Publications Citing Use of Products

    Perifosine purchased from MedChemExpress. Usage Cited in: Front Oncol. 2021 Apr 12;11:608570.  [Abstract]

    The rescue test of PI3K/Akt/mTOR signaling in response to 17α-PG in MDA-MB-453/BCRP cells. The cells are starved for 48 h and then treated with 1,000 nM 17α-PG combined with siAkt or Perifosine.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Perifosine is an oral Akt inhibitor which inhibits proliferation of different tumor cell lines with IC50s of 0.6-8.9 μM.

    IC50 & Target[1]

    Autophagy

     

    In Vitro

    The IC50 for growth of Ntv-a/LacZ cell lines is determined by MTT assay. When the cells are cultured for 48 hours in 10% FCS-supplemented media, the IC50 for cells with constitutively active PDGF, Ras, or Akt signaling is similar and found to be ~45 μM[1].Perifosine, a oral-bioavailable alkylphospholipid (ALK), on the cell cycle kinetics of immortalized keratinocytes (HaCaT) as well as head and neck squamous carcinoma cells. Proliferation is assessed by the incorporation of [3H]thymidine into cellular DNA. Exposure to Perifosine (0.1-30 μM) for 24 h results in a dose-dependent inhibition of [3H]thymidine uptake in all cell lines tested. The IC50s for growth are between 0.6 and 8.9 μM, reaching IC80s of ~10 μM. Perifosine blocks cell cycle progression of head and neck squamous carcinoma cells at G1-S and G2-M by inducing p21WAF1, irrespective of p53 function, and may be exploited clinically because the majority of human malignancies harbor p53 mutations. Perifosine (20 μM) induces both G1-S and G2-M cell cycle arrest, together with p21WAF1 expression in both p53 wild-type and p53-/- clones[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Perifosine Related Antibodies
    In Vivo

    Mice are identified with tumors by bioluminescence imaging and either treated them with 100 mg/kg Temozolomide, or 30 mg/kg Perifosine, or a combination with 100 mg/kg Temozolomide and 30 mg/kg Perifosine (Temozolomide+Perifosine) for 3 to 5 days. The mice are sacrificed and tumors analyzed histologically for cell proliferation by Ki-67 immunostaining. Ki-67 staining index is significantly reduced in mice treated with either Temozolomide (Ki-67 staining index=5.5±1.2%, n=4, P=0.0019) or Perifosine (Ki-67 staining index=3.2±1.1%, n=3, P=0.001) compared with Control, demonstrating the inhibitory effect on proliferation. Most importantly, the tumors treated with Temozolomide+Perifosine have the lowest Ki-67 staining index (1.7±1.2%, n=3, P=0.0005). The additional treatment with Perifosine results in a significantly lower proliferation rate than Temozolomide alone (P=0.0087)[1]. Perifosine markedly decreases p-Akt from 10 min to 24 hours and subsequently, moderately decreased p-S6 from 1h to 24 h after injection[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    461.66

    Formula

    C25H52NO4P
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    [O-]P(OC1CC[N+](C)(CC1)C)(OCCCCCCCCCCCCCCCCCC)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    H2O : 100 mg/mL (216.61 mM; Need ultrasonic)

    DMF : < 1 mg/mL (insoluble)

    DMSO : < 1 mg/mL (insoluble or slightly soluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1661 mL 10.8305 mL 21.6610 mL
    5 mM 0.4332 mL 2.1661 mL 4.3322 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

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    In Vivo:

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  PBS

      Solubility: 50 mg/mL (108.30 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    Purity & Documentation

    Purity: ≥98.0%

    COA (238 KB) HNMR (190 KB) LCMS (336 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [2]

    Exponentially growing cells (HN12, HN30, and HaCaT) are lysed, and 500 μg of total cellular protein are used to immunoprecipitate active cdc2 and cdk2 complexes. After capturing with gammabind G Sepharose and subsequent washes, the active immune complexes are assessed for activity in the presence of increasing concentrations of Perifosine (0.1-30 μM) or flavopiridol (300 nM) in the kinase assay buffer containing [γ-32P]ATP (3000 Ci/mmol) and 0.2 mg/mL histone H1, 25 μM ATP. Reactions are incubated at 37°C for 30 min and terminated by the addition of SDS-gel loading buffer, resolved in SDS-PAGE, and dried gels are subjected to autoradiography and phosphorimaging[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [2]

    Cell proliferation studies by measuring the uptake of [3H]thymidine is performed. Briefly, HNSCC and HaCaT cells (1-2×104/well) are grown overnight in 24-well plates and exposed to either Perifosine (0.1-30 μM) or PBS (control). After treatment (24-48 h), cells are pulsed with [3H]thymidine (1 μCi/well) for 4-6 h, fixed (5% trichloroacetic acid), and solubilized (0.5 M NaOH) before scintillation counting. Experiments are performed in triplicates[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1][3]

    Mice[1]
    Drug treatment of tumor-bearing mice. Image-positive Ef-luc Ntv-a mice are treated daily with i.p. administration of buffer alone as a control, or i.p. administration of 100 mg/kg Temozolomide, or oral administration of 30 mg/kg Perifosine, or a combination with Perifosine and Temozolomide for 3 to 5 days. The mean doses of the treatments are: Control, 5 (all five); Temozolomide, 3.75 (three to five); Perifosine, 3.75 (three to four); and Perifosine+Temozolomide, 3 (all three). Control buffer solution consisted of 5% DMSO and 1% Tween 80 in distilled water.
    Rats[3]
    To further determine whether the paradoxical effect of rapamycin on S6 phosphorylation is related to upstream signals of Akt-mTOR, rats are treated with Perifosine (20 mg/kg, ip, once), an Akt inhibitor, 30 min before rapamycin administration. Rats are sacrificed 1 h or 6 h after rapamycin injection.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O 1 mM 2.1661 mL 10.8305 mL 21.6610 mL 54.1524 mL
    5 mM 0.4332 mL 2.1661 mL 4.3322 mL 10.8305 mL
    10 mM 0.2166 mL 1.0830 mL 2.1661 mL 5.4152 mL
    15 mM 0.1444 mL 0.7220 mL 1.4441 mL 3.6102 mL
    20 mM 0.1083 mL 0.5415 mL 1.0830 mL 2.7076 mL
    25 mM 0.0866 mL 0.4332 mL 0.8664 mL 2.1661 mL
    30 mM 0.0722 mL 0.3610 mL 0.7220 mL 1.8051 mL
    40 mM 0.0542 mL 0.2708 mL 0.5415 mL 1.3538 mL
    50 mM 0.0433 mL 0.2166 mL 0.4332 mL 1.0830 mL
    60 mM 0.0361 mL 0.1805 mL 0.3610 mL 0.9025 mL
    80 mM 0.0271 mL 0.1354 mL 0.2708 mL 0.6769 mL
    100 mM 0.0217 mL 0.1083 mL 0.2166 mL 0.5415 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Perifosine Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Perifosine157716-52-4KRX-0401 NSC 639966 D21266KRX0401KRX 0401NSC639966NSC 639966NSC-639966D21266D 21266D-21266AktAutophagyApoptosisPKBProtein kinase BInhibitorinhibitorinhibit

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