Perifosine (KRX-0401)

Catalog No.S1037

Perifosine (KRX-0401) is a novel Akt inhibitor with IC50 of 4.7 μM in MM.1S cells, targets pleckstrin homology domain of Akt. Phase 3.

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Perifosine (KRX-0401) Chemical Structure

Perifosine (KRX-0401) Chemical Structure
Molecular Weight: 461.66

Validation & Quality Control

Product Use Citation(47)

Customer Product Validation(14)

Quality Control & MSDS

Related Compound Libraries

Perifosine (KRX-0401) is available in the following compound libraries:

Akt Inhibitors with Unique Features

  • Selective Akt Inhibitor

    CCT128930 AKT2-selective, IC50=6 nM.

  • Most Potent Akt Inhibitor

    AZD5363 Akt1, IC50=3 nM; Akt2, IC50=8 nM; Akt3, IC50=8 nM.

  • Akt Inhibitor in Clinical Trial

    Ipatasertib (GDC-0068) Phase II for Prostate Cancer and Gastric Cancer.

  • Newest Akt Inhibitor

    AZD5363 Potent inhibitor of all isoforms of Akt (Akt1/Akt2/Akt3) with IC50 of 3 nM/8 nM/8 nM, similar to P70S6K/PKA and lower activity towards ROCK1/2.

Product Information

  • Compare Akt Inhibitors
    Compare Akt Products
  • Research Area

Product Description

Biological Activity

Description Perifosine (KRX-0401) 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 [1]
(MM.1S cells)
IC50 4.7 μM
In vitro Perifosine develops anti-proliferative properties with IC50 of 0.6-8.9 μM in immortalized keratinocytes (HaCaT), and head and neck squamous carcinoma cells. [1] Perifosine 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. [2] Perifosine (10 μM) completely inhibits the phosphorylation of Akt in MM.1S cells. [3] A recent study demonstrates Perifosine induces cell cycle arrest and apoptosis in human hepatocellular carcinoma cell lines by blockade of Akt phosphorylation. [4]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
T24 BC MnjHSpVv[3Srb36gRZN{[Xl?MV[wMlUwOS9{LkWg{txONYfjU5pyOyCqNUnHWXEyemWmdXPld{B1cGViYnHzZYwhS0JidInyc5NqdmVicHjvd5Bpd3K7bHH0bY9vKGyndnXsd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>NF3BUoEzPjB7N{i3Ny=>
T24 BC MVXD[YxtKF[rYXLpcIl1gSCDc4PhfS=>MmnCNE42NzFxMj61JO69VQ>?MoTsNlQhcA>?MWXlcohidmOnczDzc5Ji\mWwaXKtbY5lfWOnZDDj[YxtKH[rYXLpcIl1gSCmZXPy[YF{\Q>?NHy3[pozPjB7N{i3Ny=>
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U-87 MG MXvGeY5kfGmxbjDBd5NigQ>?M2nJW|IxyqEQvF2=NVrOVXZTOjUEoHi=MX;pcoNz\WG|ZYOg[I92[mynLX3lcYJz[W6nIHLveY5lKHO2coXjeJVz\XN?NYH5RXRSOjV7M{SyN|I>
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U-87 MG NXPDbWxnTnWwY4Tpc44hSXO|YYm=MYeyNOKh|ryPM1nn[|YwOjRiaB?=Ml7RbY5kemWjc3XzJJRp\SCjdYTvdIhi\2mlIH\seZghKGG2IE[gbEB4cGmuZTDpcohq[mm2czD0bIl{KG[udYigZZQhOjSqMmXJNlU6OzR{M{K=
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Bel-7402NFzVZYNHfW6ldHnvckBCe3OjeR?=MVy1M|ExNzJyIN88US=>MoDtNlQhcA>?MknodoV{fWy2czDpckB1cGViYXPjeY12dGG2aX;uJI9nKGOnbHygcpVu[mW{IHnuJJRp\SCJMj;NJJBp[XOnM1z3blIxQDR{NEK1
HepG2 MVfBdI9xfG:|aYOgRZN{e2G7NX\0eXU{PS9zMD:yNEDPxE1?M4DqOFI1NzR6IHi=NHn4SZZqdmS3Y3XzJIFxd3C2b4Ppd{BifCC2aHWgcI9v\y22aX3lJIV5eG:|dYLlNYnlfYZtOjB6NEK0NlU>
Bel-7402M3nnfGFxd3C2b4Ppd{BCe3O|YYm=M2P4W|UwOTBxMkCg{txOM3LoS|I1NzR6IHi=NEjuNYVqdmS3Y3XzJIFxd3C2b4Ppd{BifCC2aHWgcI9v\y22aX3lJIV5eG:|dYLlM124dFIxQDR{NEK1
OAW-42NFXYPGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NFzhOmExNTRyIN88US=>MYC3NuKhcA>?NYTabmlWUUN3MI6xNEDPxE1uIHnubIljcXS|IHPlcIwh\3Kxd4ToJIlvKGFiZH;z[UBl\XCnbnTlcpQhdWGwbnXyMVSyNFQxPTJ7Nh?=
PA-1 NY\FXVI5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NET0e4gxNTRyIN88US=>MVS3NuKhcA>?NGnnRpBKSzVyfkK1JO69VSxiaX7obYJqfHNiY3XscEBoem:5dHigbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK=MW[yNFQxPTJ7Nh?=
SKOV3 MkTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NEfycYMxNTRyIN88US=>MnTyO|LDqGh?NHP0c5NKSzVyfkOwJO69VSxiaX7obYJqfHNiY3XscEBoem:5dHigbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK=M4La[lIxPDB3Mkm2
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A2780cis NEX5[otIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M2LmN|AuOjBizszNNHW3dIw1QC95MjDoNXyzRXVUUUN3MNMgQeKhPsLizsztNU\afng6OjB2MEWyPVY>
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... Click to View More Cell Line Experimental Data

In vivo Perifosine combining with temozolomide reduces tumor proliferation (a PDGF-driven gliomagenesis) in vivo. The results indicate that Perifosine is an effective drug in gliomas in which Akt and Ras-Erk 1/2 pathways are frequently activated, and may be new candidate for glima treatment in the clinic. [2] Both oral daily and weekly administration of Perifosine significantly reduce human MM tumor growth and increase survival, compared with control animals treated with PBS vehicle only. [3] Perifosine induces thrombocytosis and leukocytosis and increases myelopoiesis in murine marrow and spleen, whereas it causes apoptosis in myeloma xenografts. [5]
Features

Protocol(Only for 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 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (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).
Formulation 0.9% NaCl solution
Dosages 250 mg/kg/wk or 36 mg/kg/d
Administration Oral gavage

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
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.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Vyomesh Patel, et al. Cancer Res, 2002, 62(5), 1401-1409

[2] Momota H, et al. Cancer Res, 2005, 65(16), 7429-7435.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-05-07)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02238496 Recruiting Brain Tumor, Recurrent|Glioblastoma|Anaplastic Astrocytoma|Anaplastic Oligodendroglioma|Mixed Glioma Andrew Lassman|Pfizer|AEterna Zentaris|Columbia University July 2014 Phase 2
NCT01224730 Active, not recruiting Cancer AEterna Zentaris January 2012 Phase 1
NCT01097018 Completed Colorectal Cancer AEterna Zentaris April 2010 Phase 3
NCT01049841 Active, not recruiting Pediatric Solid Tumors Memorial Sloan Kettering Cancer Center|University of Wisc  ...more Memorial Sloan Kettering Cancer Center|University of Wisconsin, Madison|Duke University|NATL COMP CA NETWORK|Pfizer|AEterna Zentaris January 2010 Phase 1
NCT01051557 Active, not recruiting Adult Anaplastic Astrocytoma|Adult Anaplastic Oligodendroglioma|Adult Diffuse Astrocytoma|Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gl  ...more Adult Anaplastic Astrocytoma|Adult Anaplastic Oligodendroglioma|Adult Diffuse Astrocytoma|Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Adult Mixed Glioma|Adult Oligodendroglioma|Recurrent Adult Brain Neoplasm National Cancer Institute (NCI) January 2010 Phase 1|Phase 2

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Chemical Information

Download Perifosine (KRX-0401) SDF
Molecular Weight (MW) 461.66
Formula

C25H52NO4P

CAS No. 157716-52-4
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms NSC639966
Solubility (25°C) * In vitro Water 8 mg/mL (17.32 mM)
Ethanol 15 mg/mL (32.49 mM)
DMSO <1 mg/mL (<1 mM)
In vivo 30% propylene glycol, 5% Tween 80, 65% D5W 30 mg/mL
* <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.
Chemical Name Piperidinium, 4-[[hydroxy(octadecyloxy)phosphinyl]oxy]-1,1-dimethyl-, inner salt

Customer Product Validation (14)


Click to enlarge
Rating
Source Cancer Cell 2013 23, 839-52. Perifosine (KRX-0401) purchased from Selleck
Method tumor size analyse
Cell Lines
Concentrations 30 mg/kg body weight
Incubation Time 5 days
Results Animals treated with perifosine for 5 days displayed reduced tumor size relative to those treated with vehicle control.

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Rating
Source Cancer Cell 2013 23, 839-52. Perifosine (KRX-0401) purchased from Selleck
Method Western blot
Cell Lines
Concentrations 30 mg/kg body weight
Incubation Time 5 days
Results Compared to the control, tumors treated with perifosine showed low levels of phosphorylated AKT and EZH2 phosphorylation, but increased global levels of H3K27 trimethylation.

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Rating
Source Cancer Cell 2013 23, 839-52. Perifosine (KRX-0401) purchased from Selleck
Method Co-IP analysis
Cell Lines
Concentrations 30 mg/kg body weight
Incubation Time 5 days
Results AKT inhibition in vivo decreased STAT3 methylation and pY-STAT3, but increased global levels of H3K27 trimethylation.

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Rating
Source Cancer Cell 2013 23, 839-52. Perifosine (KRX-0401) purchased from Selleck
Method Immunofluorescence analyses
Cell Lines
Concentrations 30 mg/kg body weight
Incubation Time 5 days
Results Immunofluorescence analyses on tumor sections further confirmed that perifosine treatment decreased pS21 EZH2 and nuclear PY-STAT3.

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Rating
Source Cancer Res 2010 70, 9106-9117. Perifosine (KRX-0401) purchased from Selleck
Method Id1 promoter assay
Cell Lines NRP-152 cells
Concentrations 10 nmol/L
Incubation Time 2 h
Results Akt inhibitor perifosine reversed the suppressive action of LR3-IGF-I on BMP4-induced Id1 promoter activity.

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Rating
Source Mol Cell Proteomics 2012 11(12), 1898-1912 . Perifosine (KRX-0401) purchased from Selleck
Method Western Blot
Cell Lines NB4 cells
Concentrations 25 μM
Incubation Time 30 min
Results In these experiments, the presence of MLN9708 caused an accumulation of LAT2 after ODPC (Fig. B)or perifosine (Fig. C) treatment, confirming that LAT2 is degraded by proteasomes after treatment with APL.

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Rating
Source Brit J Pharmacol 2010 160, 355–366. Perifosine (KRX-0401) purchased from Selleck
Method Cell morphology examination
Cell Lines HepG2 cells
Concentrations 25 μM
Incubation Time 24 h
Results Morphological changes were found to be induced in cells treated with the different APLs such as condensation and rounding, traits of cell damage and initiation of apoptosis. Again, edelfosine and perifosine treatments affected HepG2 cells more profoundly than HePC and ErPC.

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Rating
Source Mol Carcinog 2012 ahead of print. Perifosine (KRX-0401) purchased from Selleck
Method MTT assay
Cell Lines MCF7 cells
Concentrations 0.01-1 μM
Incubation Time 48 h
Results Knockdown of BRCA1 can sensitize the MCF7 cells to Perifosine in a dose-dependent manner (Figure A). BRCA1-KD also sensitizes the MCF7 cells to dual PI3K/mTOR inhibitors, such as PI-103 or BEZ235 (Figure B, D). Another inhibitor, PIK-75 which specifically inhibits PI3Ka and PI3Kg, but not mTOR, also showed similar effects on proliferation of BRCA1-KD MCF7 cells (Figure C).

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Rating
Source Cytotechnology 2010 62, 449-460. Perifosine (KRX-0401) purchased from Selleck
Method Western blot
Cell Lines HepG2 cells, Bel-7402 cells
Concentrations 5-20 μM
Incubation Time 24 h
Results When exposed to the HepG2 cell line, perifosine reduced the levels of S473p-Akt in a dose-dependent manner. A similar pattern of inhibition was also observed in Bel-7402 cells. However, no significant changes on total Akt protein levels were observed,showing that the perifosine has no effect on total Akt protein stability.

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Rating
Source Cytotechnology 2010 62, 449-460. Perifosine (KRX-0401) purchased from Selleck
Method Morphological evaluation of apoptotic cells
Cell Lines Hepatoma cells
Concentrations 10 μM
Incubation Time 48 h
Results DAPI staining showed that the typical morphological changes, such as formation of apoptotic bodies appeared after the cells were treated for 48 h with 10 μM perifosine, whereas the control cells did not show the evident apoptotic morphological changes.

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Rating
Source Cytotechnology 2010 62, 449-460. Perifosine (KRX-0401) purchased from Selleck
Method Western blot
Cell Lines hepatoma cells
Concentrations 5-20 μM
Incubation Time 48 h
Results There is a gradual increase in caspase-3 activities in the perifosine-treated cancer cells. Cleavage of procaspase-9 into the characteristic 37/35-kDa fragments was already evident after treatment with 10μM perifosine. As caspase dependant cleavage of PARP is the prime hallmark for caspase dependent apoptosis, so we also examine the effect of perifosine on PARP. As expected, perifosine induced the cleavage of PARP in a dose dependent manner, but the level of p53 and Bcl-2 was not affected in the HepG2 cells.

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Rating
Source 2010 Zhao Jing PHD Medical College of Peking University. Perifosine (KRX-0401) purchased from Selleck
Method centrosome separation assay
Cell Lines stable transfection cells
Concentrations 1 μM
Incubation Time 6-24 h
Results "This chart showed the change of the stable transfection cells in centrosome separation after the cells were treated with perifosine(1μM) 6 hours, 12 hours and 24 hours. "C" means the control group, and "P" means the group treated with perifosine

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Rating
Source 2010 Zhao Jing PHD Medical College of Peking University . Perifosine (KRX-0401) purchased from Selleck
Method DAPI staining
Cell Lines HeLa cell
Concentrations
Incubation Time
Results "TEIF(telomerase transcriptional elements-interacting factor)gene is a novel human gene and cloned from the expression library of HeLa cell through the hTERT promoter-based yeast one-hybrid assay. And now we are trying to find the interaction between TEIF and the EGF pathway.

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Rating
Source 2010 Dr. Zhang of Tianjin Medical University. Perifosine (KRX-0401) purchased from Selleck
Method Western blot
Cell Lines T47D cells
Concentrations 0-10 nM
Incubation Time 3 h
Results

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

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  • AT13148

    AT13148 is an oral, ATP-competitive, multi-AGC kinase inhibitor with IC50 of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively. Phase 1.

  • SC79

    SC79 is a brain-penetrable Akt phosphorylation activator and an inhibitor of Akt-PH domain translocation.

  • MK-2206 2HCl

    MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM in cell-free assays, respectively; no inhibitory activities against 250 other protein kinases observed. Phase 2.

    Features:The first allosteric small molecule inhibitor of Akt to enter clinical development.

  • AZD5363

    AZD5363 potently inhibits all isoforms of Akt(Akt1/Akt2/Akt3) with IC50 of 3 nM/8 nM/8 nM in cell-free assays, similar to P70S6K/PKA and lower activity towards ROCK1/2. Phase 2.

    Features:Moderate preclinical tolerability, and PD characteristics of an AKT inhibitor. Distinct profile from other AKT inhibitors in clinical development.

  • Ipatasertib (GDC-0068)

    Ipatasertib (GDC-0068) is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5 nM/18 nM/8 nM in cell-free assays, 620-fold selectivity over PKA. Phase 2.

  • GSK690693

    GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. Phase 1.

  • A-674563

    A-674563 is an Akt1 inhibitor with Ki of 11 nM in cell-free assays, modest potent to PKA and >30-fold selective for Akt1 over PKC.

    Features:Orally bioavailable compound (achieved by replacing indole of A-443654 with phenyl moiety) and somewhat less selective for Akt over PKA than A-443654.

  • Triciribine

    Triciribine is a DNA synthesis inhibitor, also inhibits Akt in PC3 cell line and HIV-1 in CEM-SS, H9, H9IIIB, U1 cells with IC50 of 130 nM and 20 nM, respectively; does not inhibit PI3K/PDK1; 5000-fold less active in cells lacking adenosine kinase. Phase 1/2.

  • Honokiol

    Honokiol is the active principle of magnolia extract that inhibits Akt-phosphorylation and promotes ERK1/2 phosphorylation. Phase 3.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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