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

Cited by 47 publications:

14 customer reviews :

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 NFqxUVNHfW6ldHnvckBCe3OjeR?=MlXNNE42NzFxMj61JO69VQ>?NWD3NHM2OyCqNEf3ZZFz\WS3Y3XzJJRp\SCkYYPhcEBESiC2eYLvd4lv\SCyaH;zdIhwenmuYYTpc44hdGW4ZXzzJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXyNGfqSHMzPjB7N{i3Ny=>
T24 BC NHr1ZWtE\WyuIG\pZYJqdGm2eTDBd5NigQ>?MWqwMlUwOS9{LkWg{txOMnfTNlQhcA>?Mnfh[Y5p[W6lZYOgd49z[W[nbnniMYlv\HWlZXSgZ4VtdCC4aXHibYxqfHliZHXjdoVie2V?Mn3GNlYxQTd6N{O=
T24 BC NHvGe|hCeG:ydH;zbZMhSXO|c3H5MkjxNk42KM7:TR?=NUXETYp2OjRiaB?=NHXI[mF{\W6|aYTpfoV{KEKFIHPlcIx{KHSxIIPvdoFn\W6rYj3pcoR2[2WmIHHwc5B1d3SrY9MgNIn4VHYzPjB7N{i3Ny=>
HepG2M4f4R2Z2dmO2aX;uJGF{e2G7MnnHNlDDqM7:TR?=M{LRS|I1yqCqMlXUdJJw\HWlZYOgZY4hcW62ZX7z[UBkgXSxcHzhd41q[yC4YXP1c4xqgmG2aX;uJINwenKnc4DvcoRqdmdidH:gZUBvd3SjYnzlJIRqdGG2YYTpc44hd2ZidHjlJGVTKGOrc4Tldo5{MV:yOVk{PDJ|Mh?=
U-87 MG MoTySpVv[3Srb36gRZN{[Xl?M4rzdlIxyqEQvF2=NX25bopwOjUEoHi=NGrCNldqdmO{ZXHz[ZMh\G:3YnzlMY1mdWK{YX7lJIJwfW6mIIP0dpVkfHW{ZYO=NEHmRW4zPTl|NEKzNi=>
HepG2M4nzXmZ2dmO2aX;uJGF{e2G7M4rw[lIxyqEQvF2=MYm2M|I1KGh?MYrpcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iCOQ{OtTWkh[2:2cnXheIVlKHerdHigR3E>NWjIUFh2OjV7M{SyN|I>
U-87 MG MoK5SpVv[3Srb36gRZN{[Xl?MUKyNOKh|ryPMnvoOk8zPCCqNGHySWxqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjDMR|MuUUliY3;0doVifGWmIIfpeIghS1F?NXK4c45POjV7M{SyN|I>
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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 2016-07-30)

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

Tech Support

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