Perifosine (KRX-0401)

Description In vitro In vivo

Product Name: Perifosine (KRX-0401)
CAS No.: 157716-52-4
Chemical Name: Perifosine (KRX-0401)
Synonyms: CS-449;D21266;D 21266;D-21266;KRX0401;KRX 0401;KRX-0401;NSC 639966;Perifosine;KRX-0401, NKA17
CBNumber: CB21179471
Molecular Formula: C25H52NO4P
Formula Weight: 461.663
MOL File: 157716-52-4.mol

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Perifosine (KRX-0401) Property

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

WGK Germany: 3
HS Code: 2933399990

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H226Flammable liquid and vapour

Precautionary statements

P210Keep away from heat/sparks/open flames/hot surfaces. — No smoking.

P233Keep container tightly closed.

P240Ground/bond container and receiving equipment.

P241Use explosion-proof electrical/ventilating/lighting/…/equipment.

P242Use only non-sparking tools.

P243Take precautionary measures against static discharge.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P303+P361+P353IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower.

P370+P378In case of fire: Use … for extinction.

P403+P235Store in a well-ventilated place. Keep cool.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML0612
Product name: Perifosine
Purity: ≥98% (HPLC)
Packaging: 10mg
Price: $134
Updated: 2024/03/01

Sigma-Aldrich

Product number: SML0612
Product name: Perifosine
Purity: ≥98% (HPLC)
Packaging: 50mg
Price: $543
Updated: 2024/03/01

Cayman Chemical

Product number: 10008112
Product name: Perifosine
Purity: ≥98%
Packaging: 1mg
Price: $37
Updated: 2024/03/01

Cayman Chemical

Product number: 10008112
Product name: Perifosine
Purity: ≥98%
Packaging: 5mg
Price: $127
Updated: 2024/03/01

Cayman Chemical

Product number: 10008112
Product name: Perifosine
Purity: ≥98%
Packaging: 10mg
Price: $178
Updated: 2024/03/01

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Perifosine (KRX-0401) Chemical Properties,Usage,Production

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) Preparation Products And Raw materials

Raw materials

Preparation Products

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Perifosine (KRX-0401) Suppliers

Canada 1 China 138 India 2 United Kingdom 4 United States 30 Global 175

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View Lastest Price from Perifosine (KRX-0401) manufacturers

Beijing Yibai Biotechnology Co., Ltd

Product: Perifosine 157716-52-4
Price: US $0.00-0.00/KG
Min. Order: 1g
Purity: 99.0%
Supply Ability: 500kg/month
Release date: 2019-08-28

Career Henan Chemical Co

Product: Perifosine (KRX-0401) 157716-52-4
Price: US $2.00/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: 100kg
Release date: 2018-12-23

157716-52-4, Perifosine (KRX-0401)Related Search:

MK-2206 2HCl WORTMANNIN GDC-0068 LY 294002 HYDROCHLORIDE Rapamycin BEZ235 (NVP-BEZ235, Dactolisib) OCTADECYL PHOSPHATE Perifosine (KRX-0401) ammonium hexadecyl hydrogen phosphate

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

KRX0401; KRX 0401

CS-449

NSC 639966

Perifosine(KRX-0401)

D 21266

D21266

D-21266

KRX 0401

KRX0401

KRX-0401

Perifosine (NSC-639966)

1,1-diMethylpiperidiniuM-4-yl octadecyl phosphate

KRX-0401, NKA17

Piperidinium, 4-[[hydroxy(octadecyloxy)phosphinyl]oxy]-1,1-dimethyl-, inner salt

Octadecyl-(1,1-dimethyl-4-piperidylio) phosphate

Perifosine, >=98%

Perifosine, 98%, an oral Akt inhibitor

KRX-0401; NSC 639966;D-21266;KRX 0401;KRX0401;D21266;D 21266

Perifosine (KRX-0401) USP/EP/BP

Perifosine KRX-0401 KRX0401

Perifosine, Akt inhibitor

157716-52-4

C25H52NO4P

PI3K/Akt/mTOR

Antineoplastic

Akt

mTOR

PI3K

Inhibitors

Intermediates & Fine Chemicals

Pharmaceuticals