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Perifosine (KRX-0401)

Basic information Description In vitro In vivo Safety Supplier Related

Perifosine (KRX-0401) Basic information

Product Name:
Perifosine (KRX-0401)
Synonyms:
  • Perifosine
  • (1,1-Dimethylpiperidin-1-ium-4-yl) octadecyl phosphate
  • 4-((Hydroxy(octadecyloxy)phosphinyl)oxy)-1,1-dimethylpiperidinium inner salt
  • Perifosine,D 21266
  • 4-[[Hydroxy(octadecycloxy)phosphinyl]oxy]-1,1-diMethylpiperidiniuM inner salt
  • D-21266 octadecyl-(N,N-diMethyl-piperidino-4-yl)-phosphate
  • Perifosine【(1,1-dimethylpiperidin-1-ium-4-yl) octadecyl phosphate】
  • Perifosine - KRX 0401 | D 21266
CAS:
157716-52-4
MF:
C25H52NO4P
MW:
461.663
EINECS:
690-653-3
Product Categories:
  • PI3K/Akt/mTOR
  • Antineoplastic
  • Inhibitors
  • Akt
  • mTOR
  • PI3K
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
Mol File:
157716-52-4.mol
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Perifosine (KRX-0401) Chemical Properties

Melting point:
271-272° (dec)
storage temp. 
-20°C
solubility 
H2O: soluble10mg/mL, clear
form 
powder
color 
white to beige
InChIKey
SZFPYBIJACMNJV-UHFFFAOYSA-N
CAS DataBase Reference
157716-52-4
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Safety Information

WGK Germany 
3
HS Code 
2933399990
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Perifosine (KRX-0401) Usage And Synthesis

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.

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. 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.  Perifosine (10 μM) completely inhibits the phosphorylation of Akt in MM.1S cells. A recent study demonstrates Perifosine induces cell cycle arrest and apoptosis in human hepatocellular carcinoma cell lines by blockade of Akt phosphorylation.

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.  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. Perifosine induces thrombocytosis and leukocytosis and increases myelopoiesis in murine marrow and spleen, whereas it causes apoptosis in myeloma xenografts.

Uses

Antineoplastic.

Uses

An alkylphospholipid which inhibits Akt activation and the anti-apoptotic MAPK pathway.

Uses

It acts as an Akt inhibitor and a PI3K inhibitor, and is a drug candidate being developed for a variety of cancer indications.

Definition

ChEBI: A phospholipid consisting of 1,1-dimethylpiperidinium-4-yl hydrogen phosphate in which the hydrogen is replaced by a stearyl (octadecyl) group.

Biological Activity

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].

Biochem/physiol Actions

Perifosine (octadecyl-(1,1-dimethyl-4-piperidylio)) is an antitumor compound. It acts at lipid rafts and stops lysosomal accumulation and mTORC1 (mammalian target of rapamycin complex 1) signaling. This drug exhibits significant antiproliferative activity in vitro and in vivo in various human cancer model systems.

target

AKT

storage

Store at -20°C

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.

Perifosine (KRX-0401)Supplier

Shanghai Yuanding Chem. Sci. & Tech. Co., Ltd. Gold
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Product Name:Perifosine
CAS:157716-52-4
Purity:97% Package:1g,5g,10g,100g,1kg
Shanghai Boyle Chemical Co., Ltd.
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Product Name:Perifosine
CAS:157716-52-4
J & K SCIENTIFIC LTD.
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010-82848833 400-666-7788
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Product Name:Perifosine, 98%, an oral Akt inhibitor
CAS:157716-52-4
Purity:98% Package:10MG;5MG
Yangzhou Siyu Chemical Co.,Ltd.
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0514-87325867
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Product Name:Perifosine
CAS:157716-52-4
Purity:98% Package:1g;5g;10g;25g;50g;100g
Chembest Research Laboratories Limited
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+86-21-20908456
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Product Name:Perifosine(KRX-0401)
CAS:157716-52-4
Remarks:C13999