Perifosine (KRX-0401)

Bezeichnung:Perifosine (KRX-0401)

CAS-Nr157716-52-4

Englisch Name:Perifosine (KRX-0401)

CBNumberCB21179471

SummenformelC25H52NO4P

Molgewicht461.663

MOL-Datei157716-52-4.mol

Perifosine (KRX-0401) physikalisch-chemischer Eigenschaften

Schmelzpunkt	271-272° (dec)
storage temp.	-20°C
Löslichkeit	H2O: soluble10mg/mL, clear
Aggregatzustand	powder
Farbe	white to beige
InChIKey	SZFPYBIJACMNJV-UHFFFAOYSA-N
CAS Datenbank	157716-52-4

Sicherheit

WGK Germany	3
HS Code	2933399990

Gefahreninformationscode (GHS)

Perifosine (KRX-0401) Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
An alkylphospholipid which inhibits Akt activation and the anti-apoptotic MAPK pathway.
Verwenden
Antineoplastic.
Verwenden
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.
Biologische Aktivität
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
Lager
Store at -20°C
Einzelnachweise
[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) Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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