Perifosine

Catalog No.S1037 Batch:S103706

Print

Technical Data

Formula

C25H52NO4P
Molecular Weight 461.66 CAS No. 157716-52-4
Solubility (25°C)* In vitro Water 92 mg/mL (199.28 mM)
Ethanol 92 mg/mL (199.28 mM)
DMSO Insoluble
In Vivo (Add solvents to the product individually and in order.)
Clear solution
water

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 8.000mg/ml (17.33mM) Taking the 1 mL working solution as an example, add 8 mg of this product to 1 ml of ddH2O, mix evenly to make it clear, The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Perifosine is a novel Akt inhibitor with IC50 of 4.7 μM in MM.1S cells, targets pleckstrin homology domain of Akt. Phase 3.
Targets
Akt
(MM.1S cells)
4.7 μM
In vitro

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

In Vivo

Perifosine in combination reduces tumour proliferation (a PDGF-driven gliomagenesis) in vivo. The results indicate that this compound is an effective drug in gliomas in which Akt and Ras-Erk 1/2 pathways are frequently activated, and may be a new candidate for glioma treatment in the clinic. Both oral daily and weekly administration of this chemical significantly reduce human MM tumour growth and increase survival, compared with control animals treated with PBS vehicle only. It induces thrombocytosis and leucocytosis and increases myelopoiesis in murine marrow and spleen, whereas it causes apoptosis in myeloma xenografts.

Protocol (from reference)

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

  • Method

    Cells are incubated in the medium with 10% FCS for 48 hours with indicated concentration of Periosine. Cell viability is determined by the 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).

  • Dosages

    250 mg/kg/wk or 36 mg/kg/d

  • Administration

    Oral gavage

References

  • https://pubmed.ncbi.nlm.nih.gov/11888912/
  • http://www.ncbi.nlm.nih.gov/pubmed?term=16103096
  • http://www.ncbi.nlm.nih.gov/pubmed?term=16418332%20
  • https://pubmed.ncbi.nlm.nih.gov/20842425/
  • https://pubmed.ncbi.nlm.nih.gov/17588472/

Customer Product Validation

Tumor growth of 827 GSC-derived xenograftstreated with an AKT inhibitor perifosine (30 mg/kgbody weight). Twenty-three days after tumorimplantation in mice, perifosine was administeredby intraperitoneal injection (daily for 5 days). Errorbars represent SD. Five mice per group, *p < 0.01.

Data from [ Cancer Cell , 2013 , 23, 839-52 ]

Immunoblot analysis of pY-STAT3, EZH2, AKT,and trimethylated H3K27 in lysates from xenografttumors treated with an AKT inhibitor perifosine.

Data from [ Cancer Cell , 2013 , 23, 839-52 ]

Co-IP analysis of methylated STAT3 in GBM xenograft tumors treated with perifosine.AKT inhibition in vivodecreased STAT3 methylation and pY-STAT3, but increased global levels of H3K27 trimethylation.

Data from [ Cancer Cell , 2013 , 23, 839-52 ]

IF staining of pS21 EZH2 and pY-STAT3 on the frozen sections of GBM xenografts treated with vehicle or perifosine. Nuclei were stained with DAPI. Bar represents 10 microns.

Data from [ Cancer Cell , 2013 , 23, 839-52 ]

Sellecks Perifosine Has Been Cited by 176 Publications

CD22 modulation alleviates amyloid β-induced neuroinflammation [ J Neuroinflammation, 2025, 22(1):32] PubMed: 39910617
Low-Dose Perifosine, a Phase II Phospholipid Akt Inhibitor, Selectively Sensitizes Drug-Resistant ABCB1-Overexpressing Cancer Cells [ Biomol Ther (Seoul), 2025, 33(1):170-181] PubMed: 39632683
Patient-derived rhabdomyosarcoma cells recapitulate the genetic and transcriptomic landscapes of primary tumors [ iScience, 2024, 27(10):110862] PubMed: 39319271
RANK/RANKL axis promotes migration, invasion, and metastasis of osteosarcoma via activating NF-κB pathway [ Exp Cell Res, 2024, 436(2):113978] PubMed: 38382805
TRIB1 confers therapeutic resistance in GBM cells by activating the ERK and Akt pathways [ Sci Rep, 2023, 13(1):12424] PubMed: 37528172
Deficiency of lipopolysaccharide binding protein facilitates adipose browning, glucose uptake and oxygen consumption in mouse embryonic fibroblasts via activating PI3K/Akt/mTOR pathway and inhibiting autophagy [ Cell Cycle, 2023, 1-19.] PubMed: 36710409
Synthesis of N-oxyamide analogues of protein kinase B (Akt) targeting anionic glycoglycerolipids and their antiproliferative activity on human ovarian carcinoma cells [ Org Biomol Chem, 2023, 21(32):6572-6587] PubMed: 37526931
Ceramide kinase confers tamoxifen resistance in estrogen receptor-positive breast cancer by altering sphingolipid metabolism [ Pharmacol Res, 2022, 187:106558] PubMed: 36410675
(+)-Cyanidan-3-ol inhibits epidermoid squamous cell carcinoma growth via inhibiting AKT/mTOR signaling through modulating CIP2A-PP2A axis [ Phytomedicine, 2022, 101:154116] PubMed: 35525235
In Vitro Angiogenesis Inhibition and Endothelial Cell Growth and Morphology [ Int J Mol Sci, 2022, 23(8)4277] PubMed: 35457095

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.