Perifosine

製品コードS1037 バッチS103706

印刷

化学情報

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）

Clear solution

water

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

8.000mg/ml (17.33mM)

Taking the 1 mL working solution as an example, add 8 mg of this product to 1 ml of ddH2O, mix evenly to make it clear, The mixed solution should be used immediately for optimal results.

* <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] This compound 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] It completely inhibits the phosphorylation of Akt in MM.1S cells. ^[3] A recent study demonstrates this chemical induces cell cycle arrest and apoptosis in human hepatocellular carcinoma cell lines by blockade of Akt phosphorylation. ^[4]
in vivo	Perifosine in combination reduces tumor proliferation (a PDGF-driven gliomagenesis) in vivo. The results indicate that this compound 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 this chemical significantly reduce human MM tumor growth and increase survival, compared with control animals treated with PBS vehicle only. ^[3] It 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
キナーゼアッセイ	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 the 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

参考

https://pubmed.ncbi.nlm.nih.gov/11888912/
http://www.ncbi.nlm.nih.gov/pubmed?term=16103096
http://www.ncbi.nlm.nih.gov/pubmed?term=16418332%20

https://pubmed.ncbi.nlm.nih.gov/20842425/
https://pubmed.ncbi.nlm.nih.gov/17588472/

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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：

CD22 modulation alleviates amyloid β-induced neuroinflammation [ J Neuroinflammation, 2025, 22(1):32]	PubMed: 39910617
Low-Dose Perifosine, a Phase II Phospholipid Akt Inhibitor, Selectively Sensitizes Drug-Resistant ABCB1-Overexpressing Cancer Cells [ Biomol Ther (Seoul), 2025, 33(1):170-181]	PubMed: 39632683
Patient-derived rhabdomyosarcoma cells recapitulate the genetic and transcriptomic landscapes of primary tumors [ iScience, 2024, 27(10):110862]	PubMed: 39319271
RANK/RANKL axis promotes migration, invasion, and metastasis of osteosarcoma via activating NF-κB pathway [ Exp Cell Res, 2024, 436(2):113978]	PubMed: 38382805
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

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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