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Perifosine | Akt/PI3K inhibitor

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Price:
$109.00
Catalog #:
C7374-5
Quantity:


Product Description

Perifosine (KRX-0401) is an orally bioavailable Akt and PI3K inhibitor of the alkylphospholipid class. Unlike ATP binding kinase inhibitors, perifosine targets the pleckstrin homology domain of Akt, thus preventing its translocation to the plasma membrane. Though structurally similar to miltefosine and edelfosine, it has improved bioavailability and less GI side effects. It has orphan drug status in the United States for the treatment of multiple myeloma and neuroblastoma. In multiple myeloma cell lines, perifosine showed significant dose-dependent growth inhibition with an IC50 of 1 to 12.5 uM. [4] In PC-3 cells Perifosine inhibits Akt phosphorylation on Thr308 and Ser473 without affecting the amount of Akt. Perifosine has been shown to promote cell cycle arrest at either G1-S or G2-M phases with upregulation of p21 in a p53-independent manner. [1]

Perifosine targets the lipid-binding PH domain and inhibits translocation of Akt to the cell membrane. It decreases Akt phosphorylation and increases caspase-dependent apoptosis in neuroblastoma cell lines. [2] Recent combination studies with mTOR inhibitor temsirolimus have shown perifosine to be synergistic. Perifosine also has been shown to sensitize breast cancer stem cells to radiation. [3]


Technical information:

Chemical Formula:   C25H52NO4P
CAS #:   157716-52-4
Molecular Weight:   461.66
Purity:   >98%
Appearance:   Pale Yellow
Chemical Name:   Piperidinium, 4-[[hydroxy(octadecyloxy)phosphinyl]oxy]-1,1-dimethyl-, inner salt
Solubility:   Up to 100 mM in water in DMSO
Synonyms:   KRX-0401, KRX0401, Perifosine, NSC-639966, NSC 639966, NSC639966

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1. Kondapaka et al., Perifosine, a novel alkylphospholipid, inhibits protein kinase B activation. Mol. Cancer Ther. 2003, 2, 1093-1103. Pubmed ID: 14617782
2. Sun et al., Emerging treatment options for the treatment of neuroblastoma: potential role of perifosine. OncoTargets and Therapy 2012, 5, 21-29. Pubmed ID: 22419878
3. Venkatesha et al., Sensitization of pancreatic cancer stem cells to gemcitabine by Chk1 inhibition. Neoplasia 2012, 14(6), 519-525. Pubmed ID: 22787433
4. Hideshima et al, Perifosine, an oral bioactive novel alkylphospholipid, inhibits Akt and induces in vitro and in vivo cytotoxicity in human multiple myeloma cells. Blood 2006, 107(10), 4053-4062. Pubmed ID: 22419878

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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