Perifosine

製品コードS1037 バッチS103702

印刷

化学情報

Chemical Structure Synonyms KRX-0401, NSC639966, D21266 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C25H52NO4P
分子量 461.66 CAS No. 157716-52-4
Solubility (25°C)* 体外 Ethanol 15 mg/mL (32.49 mM)
Water 8 mg/mL (17.32 mM)
DMSO Insoluble
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Perifosine 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. [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]
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]

プロトコル(参考用のみ)

キナーゼアッセイ 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.
細胞アッセイ 細胞株 Human glioma cell lines
濃度 0, 15, 30 and 45 μM
反応時間 48 hours
実験の流れ 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.
動物実験 動物モデル MM.1S MM cells are inoculated subcutaneously in the right flank of Beige-nude-xid (BNX) mice (5 to 6 weeks old).
投薬量 250 mg/kg/wk or 36 mg/kg/d
投与方法 Oral gavage

カスタマーフィードバック

Data from [Data independently produced by Cancer Cell, 2013, 23, 839-52]

Data from [Data independently produced by Cancer Cell, 2013, 23, 839-52]

Data from [Data independently produced by Cancer Cell, 2013, 23, 839-52]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

TRIB1 confers therapeutic resistance in GBM cells by activating the ERK and Akt pathways [ Sci Rep, 2023, 13(1):12424] PubMed: 37528172
TRIB1 confers therapeutic resistance in GBM cells by activating the ERK and Akt pathways [ Sci Rep, 2023, 13(1):12424] PubMed: 37528172
Deficiency of lipopolysaccharide binding protein facilitates adipose browning, glucose uptake and oxygen consumption in mouse embryonic fibroblasts via activating PI3K/Akt/mTOR pathway and inhibiting autophagy [ Cell Cycle, 2023, 1-19.] PubMed: 36710409
Synthesis of N-oxyamide analogues of protein kinase B (Akt) targeting anionic glycoglycerolipids and their antiproliferative activity on human ovarian carcinoma cells [ Org Biomol Chem, 2023, 21(32):6572-6587] PubMed: 37526931
Ceramide kinase confers tamoxifen resistance in estrogen receptor-positive breast cancer by altering sphingolipid metabolism [ Pharmacol Res, 2022, 187:106558] PubMed: 36410675
(+)-Cyanidan-3-ol inhibits epidermoid squamous cell carcinoma growth via inhibiting AKT/mTOR signaling through modulating CIP2A-PP2A axis [ Phytomedicine, 2022, 101:154116] PubMed: 35525235
In Vitro Angiogenesis Inhibition and Endothelial Cell Growth and Morphology [ Int J Mol Sci, 2022, 23(8)4277] PubMed: 35457095
The Significance of p-AKT1 as a Prognostic Marker and Therapeutic Target in Patients With Hormone Receptor-Positive and Human Epidermal Growth Factor Receptor-2-Positive Early Breast Cancer [ J Breast Cancer, 2022, 25(5:387-403)] PubMed: 36314765
Inhibition of cytoplasmic EZH2 induces antitumor activity through stabilization of the DLC1 tumor suppressor protein [ Nat Commun, 2021, 12(1):6941] PubMed: 34862367
Gm364 coordinates MIB2/DLL3/Notch2 to regulate female fertility through AKT activation [ Cell Death Differ, 2021, 10.1038/s41418-021-00861-5] PubMed: 34635817

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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