Perifosine

Akt inhibitor CAS# 157716-52-4

Perifosine

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Chemical structure

Perifosine

3D structure

Chemical Properties of Perifosine

Cas No. 157716-52-4 SDF Download SDF
PubChem ID 148177 Appearance Powder
Formula C25H52NO4P M.Wt 461.67
Type of Compound N/A Storage Desiccate at -20°C
Synonyms KRX-0401; NSC 639966; D21266
Solubility H2O : ≥ 153.33 mg/mL (332.13 mM)
DMF : < 1 mg/mL (insoluble)
DMSO : < 1 mg/mL (insoluble or slightly soluble)
*"≥" means soluble, but saturation unknown.
Chemical Name (1,1-dimethylpiperidin-1-ium-4-yl) octadecyl phosphate
SMILES CCCCCCCCCCCCCCCCCCOP(=O)([O-])OC1CC[N+](CC1)(C)C
Standard InChIKey SZFPYBIJACMNJV-UHFFFAOYSA-N
Standard InChI 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
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Perifosine

DescriptionPerifosine (KRX-0401) is a novel inhibitor of Akt with IC50 of 4.7 μM.
TargetsAKT    
IC504.7 μM     

Protocol

Cell experiment: [1]

Cell lines

CRW22RV1 cells

Preparation method

The solubility of this compound in DMSO is <10 mm. general tips for obtaining a higher concentration: please warm the tube at 37 °c 10 minutes and>

Reacting condition

10 μM, 24 hours

Applications

To assess the effect of perifosine on radiation-induced apoptosis, the Annexin-FITC based flow cytometry analysis was used. Both nuclear fragmentations with PI staining and translocated membrane phosphatidylserine (PS) with Annexin V staining were measured. Both perifosine and radiation induced significant apoptotic responses as shown by the increase of apoptotic cells. When radiation (6Gy) and perifosine (10 μM) were combined, the number of apoptotic cells was significantly increased. Perifosine alone did not induce cell cycle arrest at the G2/M phases and perifosine did not affect the IR-induced G2/M checkpoint.

Animal experiment: [1]

Animal models

Male Athymic Nude-Foxn1nu mice injected with CRW22RV1 cells

Dosage form

Oral administration, in a loading dose of 300 mg/kg (2 × 150 mg/kg separated by 12 hours) followed by daily maintenance doses of 35 mg/kg for 5 days

Application

Mice were separated into 4 groups: control, perifosine, radiotherapy and combined therapy. Perifosine alone did not have a significant effect on tumor growth. However, perifosine can significantly increase radiation induced tumor growth delay. To reach the 10-fold size of tumor volume to the initial volume in the control, it took 15, 19, 41 and 59 days in control, perifosine only, radiation only and combined treatment groups, respectively. It is noted that the combined treatment led to a complete remission of the CWR22RV1 tumor.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Gao Y, Ishiyama H, Sun M, et al. The alkylphospholipid, perifosine, radiosensitizes prostate cancer cells both in vitro and in vivo. Radiation oncology (London, England), 2011, 6: 39.

Perifosine Dilution Calculator

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Perifosine Molarity Calculator

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Preparing Stock Solutions of Perifosine

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.166 mL 10.8302 mL 21.6605 mL 43.321 mL 54.1512 mL
5 mM 0.4332 mL 2.166 mL 4.3321 mL 8.6642 mL 10.8302 mL
10 mM 0.2166 mL 1.083 mL 2.166 mL 4.3321 mL 5.4151 mL
50 mM 0.0433 mL 0.2166 mL 0.4332 mL 0.8664 mL 1.083 mL
100 mM 0.0217 mL 0.1083 mL 0.2166 mL 0.4332 mL 0.5415 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Perifosine

Perifosine is an inhibitor of Akt [1].

Perifosine is a synthetic antitumor alkylphospholipid. It 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. In mice inoculated with MM.1S cells, oral administration of perifosine significantly reduced MM tumor growth and increased survival [1, 2].

References:
[1] Elrod H A, Lin Y D, Yue P, et al. The alkylphospholipid perifosine induces apoptosis of human lung cancer cells requiring inhibition of Akt and activation of the extrinsic apoptotic pathway. Molecular cancer therapeutics, 2007, 6(7): 2029-2038.
[2] Hideshima T, Catley L, Yasui H, 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.

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References on Perifosine

Perifosine Mechanisms of Action in Leishmania Species.[Pubmed:28096161]

Antimicrob Agents Chemother. 2017 Mar 24;61(4). pii: AAC.02127-16.

Here the mechanism by which Perifosine induced cell death in Leishmania donovani and Leishmania amazonensis is described. The drug reduced Leishmania mitochondrial membrane potential and decreased cellular ATP levels while increasing phosphatidylserine externalization. Perifosine did not increase membrane permeabilization. We also found that the drug inhibited the phosphorylation of Akt in the parasites. These results highlight the potential use of Perifosine as an alternative to miltefosine against Leishmania.

Proteome and Acetylome Analysis Identifies Novel Pathways and Targets Regulated by Perifosine in Neuroblastoma.[Pubmed:28165023]

Sci Rep. 2017 Feb 6;7:42062.

Perifosine, an Akt inhibitor, has been shown to be effective in controlling neuroblastoma tumor growth. However, studies indicate that in addition to the ability to inhibit Akt, other mechanisms contribute to Perifosine's anti-tumor activity. To gain insight into Perifosine anti-tumor activity in neuroblastoma we have studied changes in the proteome and acetylome after Perifosine treatment in SK-N-AS neuroblastoma cells using SILAC labeling, affinity enrichment, high-resolution and LC-MS/MS analysis. Bioinformatic analysis indicates that, a total of 5,880 proteins and 3,415 lysine acetylation sites were quantified in SK-N-AS cells and 216 differentially expressed proteins and 115 differentially expressed lysine acetylation sites were obtained. These differentially expressed proteins and lysine acetylated proteins were involved in a number of different biological functions, metabolic pathways and pathophysiological processes. This study details the impact of Perifosine on proteome and lysine acetylome in SK-N-AS cells and expands our understanding of the mechanisms of Perifosine action in neuroblastoma.

A phase I study of perifosine with temsirolimus for recurrent pediatric solid tumors.[Pubmed:28035748]

Pediatr Blood Cancer. 2017 Jul;64(7).

BACKGROUND: The PI3K/AKT/mTOR pathway is aberrantly activated in many pediatric solid tumors including gliomas and medulloblastomas. Preclinical data in a pediatric glioma model demonstrated that the combination of Perifosine (AKT inhibitor) and temsirolimus (mTOR inhibitor) is more potent at inhibiting the axis than either agent alone. We conducted this study to assess pharmacokinetics and identify the maximum tolerated dose for the combination. PROCEDURE: We performed a standard 3+3 phase I, open-label, dose-escalation study in patients with recurrent/refractory pediatric solid tumors. Four dose levels of Perifosine (25-75 mg/m(2) /day) and temsirolimus (25-75 mg/m(2) IV weekly) were investigated. RESULTS: Twenty-three patients (median age 8.5 years) with brain tumors (diffuse intrinsic pontine glioma [DIPG] n = 8, high-grade glioma n = 6, medulloblastoma n = 2, ependymoma n = 1), neuroblastoma (n = 4), or rhabdomyosarcoma (n = 2) were treated. The combination was generally well tolerated and no dose-limiting toxicity was encountered. The most common grade 3 or 4 toxicities (at least possibly related) were thrombocytopenia (38.1%), neutropenia (23.8%), lymphopenia (23.8%), and hypercholesterolemia (19.0%). Pharmacokinetic findings for temsirolimus were similar to those observed in the temsirolimus single-agent phase II pediatric study and pharmacokinetic findings for Perifosine were similar to those in adults. Stable disease was seen in 9 of 11 subjects with DIPG or high-grade glioma; no partial or complete responses were achieved. CONCLUSIONS: The combination of these AKT and mTOR inhibitors was safe and feasible in patients with recurrent/refractory pediatric solid tumors.

A phase I/Ib trial targeting the Pi3k/Akt pathway using perifosine: Long-term progression-free survival of patients with resistant neuroblastoma.[Pubmed:27649927]

Int J Cancer. 2017 Jan 15;140(2):480-484.

AKT plays a pivotal role in driving the malignant phenotype of many cancers, including high-risk neuroblastoma (HR-NB). AKT signaling, however, is active in normal tissues, raising concern about excessive toxicity from its suppression. The oral AKT inhibitor Perifosine showed tolerable toxicity in adults and in our phase I trial in children with solid tumors (clinicaltrials.gov NCT00776867). We now report on the HR-NB experience. HR-NB patients received Perifosine 50-75 mg m(-2) day(-1) after a loading dose of 100-200 mg m(-2) on day 1, and continued on study until progressive disease. The 27 HR-NB patients included three treated for primary refractory disease and 24 with disease resistant to salvage therapy after 1-5 (median 2) relapses; only one had MYCN-amplified HR-NB. Pharmacokinetic studies showed muM concentrations consistent with cytotoxic levels in preclinical models. Nine patients (all MYCN-non-amplified) remained progression-free through 43+ to 74+ (median 54+) months from study entry, including the sole patient to show a complete response and eight patients who had persistence of abnormal (123) I-metaiodobenzylguanidine skeletal uptake but never developed progressive disease. Toxicity was negligible in all 27 patients, even with the prolonged treatment (11-62 months, median 38) in the nine long-term progression-free survivors. The clinical findings (i) confirm the safety of therapeutic serum levels of an AKT inhibitor in children; (ii) support Perifosine for MYCN-non-amplified HR-NB as monotherapy after completion of standard treatment or combined with other agents (based on preclinical studies) to maximize antitumor effects; and (iii) highlight the welcome possibility that refractory or relapsed MYCN-non-amplified HR-NB is potentially curable.

Description

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

Keywords:

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