受注:045-509-1970 |
技術サポート:[email protected] 平日9:00〜18:00 1営業日以内にご連絡を差し上げます |
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 | Water | 92 mg/mL (199.28 mM) | ||||
Ethanol | 92 mg/mL (199.28 mM) | ||||||
DMSO | Insoluble | ||||||
体内 (毎回新しく調製した物を用意してください) |
|
||||||
* <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. |
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] |
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 |
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]
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。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。