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Perifosine

Cat. No. M1823
Perifosine Structure
Synonym:

KRX-0401, NKA17

Size Price Availability Quantity
5mg USD 70 In stock
10mg USD 110 In stock
50mg USD 320 In stock
100mg USD 450 In stock
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Quality Control
Biological Activity

Perifosine is a novel p.o. bioavailable alkylphospholipid. Perifosine has displayed significant antiproliferative activity in vitro and in vivo in several human tumor model systems and has recently entered phase I clinical trials. Perifosine causes dose-dependent inhibition of protein kinase B/Akt phosphorylation and thus activation at concentrations causing growth inhibition of PC-3 prostate carcinoma cells. Only the myristoylated form of Akt (MYR-Akt), which bypasses the requirement for pleckstrin homology (PH) domain-mediated membrane recruitment, abrogated perifosine-mediated decrease of Akt phosphorylation and cell growth inhibition by perifosine. Perifosine decreases the plasma membrane localization of Akt, and this is substantially relieved by MYR-Akt along with relief of downstream compound effect on induction of p21(WAF1/CIP1). Perifosine does not directly affect phosphoinositide 3-kinase (PI3K), phosphoinositide-dependent kinase 1, or Akt activity at concentrations inhibiting Akt phosphorylation and membrane localization.

Protocol
Cell Experiment
Cell lines MM cells
Preparation method Growth inhibition assay. The inhibitory effect of perifosine, alone or combined with other agents, on MM cell growth was assessed by measuring 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrasodium bromide (MTT; Chemicon International, Temecula, CA) dye absorbance. Cells were pulsed with 10 μL of 5 mg/mL MTT to each well for the last 4 hours of 24-hour and/or 48-hour cultures, followed by 100 μL isopropanol containing 0.04 N HCl. Absorbance was measured at 570/630 nm using a spectrophotometer (Molecular Devices, Sunnyvale, CA).
Concentrations 0~100 μM
Incubation time 24 or 48 h
Animal Experiment
Animal models MM.1S cells xenograft model in Immunodeficient BNX mice
Formulation 0.9% sodium chloride
Dosages daily (36 mg/kg) or weekly (250 mg/kg)
Administration oral
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 461.66
Formula C25H52NO4P
CAS Number 157716-52-4
Purity >99%
Solubility Ethanol ≥90 mg/mL
Storage at -20°C
References

Perifosine , an oral, anti-cancer agent and inhibitor of the Akt pathway: mechanistic actions, pharmacodynamics, pharmacokinetics, and clinical activity.
Richardson PG, et al. Expert Opin Drug Metab Toxicol. 2012 May;8(5):623-33. PMID: 22512706.

Perifosine downregulates MDR1 gene expression and reverses multidrug-resistant phenotype by inhibiting PI3K/Akt/NF-κB signaling pathway in a human breast cancer cell line.
Lin X, et al. Neoplasma. 2012;59(3):248-56. PMID: 22329846.

Perifosine plus bortezomib and dexamethasone in patients with relapsed/refractory multiple myeloma previously treated with bortezomib: results of a multicenter phase I/II trial.
Richardson PG, et al. J Clin Oncol. 2011 Nov 10;29(32):4243-9. PMID: 21990396.

Perifosine, an oral bioactive novel alkylphospholipid, inhibits Akt and induces in vitro and in vivo cytotoxicity in human multiple myeloma cells.
Hideshima T, et al. Blood. 2006 May 15;107(10):4053-62. PMID: 16418332.

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  Catalog
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Keywords: Perifosine, KRX-0401, NKA17 supplier, Akt, inhibitors

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