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| 化学名: | PERIFOSINE | | 英語化学名: | Perifosine (KRX-0401) | | 别名: | 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;NSC 639966;Perifosine(KRX-0401) | | CAS番号: | 157716-52-4 | | 分子式: | C25H52NO4P | | 分子量: | 461.663 | | EINECS: | 690-653-3 | | カテゴリ情報: | PI3K/Akt/mTOR;Antineoplastic;Akt;mTOR;PI3K;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals | | Mol File: | 157716-52-4.mol |  |
| 融点 | 271-272° (dec) | | 貯蔵温度 | -20°C | | 溶解性 | H2O: soluble10mg/mL, clear | | 外見 | powder | | 色 | white to beige | | InChIKey | SZFPYBIJACMNJV-UHFFFAOYSA-N | | CAS データベース | 157716-52-4 |
| WGK Germany | 3 | | HSコード | 2933399990 |
| | PERIFOSINE Usage And Synthesis |
| 溶解性 | In vitro (25℃) DMSO ＜1 mg/mL (＜1 mM) | | 使用 | An alkylphospholipid which inhibits Akt activation and the anti-apoptotic MAPK pathway. | | 使用 | Antineoplastic. | | 使用 | It acts as an Akt inhibitor and a PI3K inhibitor, and is a drug candidate being developed for a variety of cancer indications. | | 定義 | ChEBI: A phospholipid consisting of 1,1-dimethylpiperidinium-4-yl hydrogen phosphate in which the hydrogen is replaced by a stearyl (octadecyl) group. | | 生物活性 | 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 | | 貯蔵 | Store at -20°C | | 参考文献 | [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. |
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