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  • Perifosine (KRX-0401)

    Perifosine (KRX-0401)

    Perifosine (KRX-0401)
    产品编号 CFN60016
    CAS编号 157716-52-4
    分子式 = 分子量 C25H52NO4P = 461.66
    产品纯度 >=98%
    物理属性 Powder
    化合物类型 Alkaloids
    植物来源
    ChemFaces的产品在影响因子大于5的优秀和顶级科学期刊中被引用
    提供自定义包装
    产品名称 产品编号 CAS编号 包装 QQ客服
    Perifosine (KRX-0401) CFN60016 157716-52-4 1mg QQ客服:2159513211
    Perifosine (KRX-0401) CFN60016 157716-52-4 5mg QQ客服:2159513211
    Perifosine (KRX-0401) CFN60016 157716-52-4 10mg QQ客服:2159513211
    Perifosine (KRX-0401) CFN60016 157716-52-4 20mg QQ客服:2159513211
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    ChemFaces的产品在许多优秀和顶级科学期刊中被引用

    Cell. 2018 Jan 11;172(1-2):249-261.e12.
    doi: 10.1016/j.cell.2017.12.019.
    IF=36.216(2019)

    PMID: 29328914

    Cell Metab. 2020 Mar 3;31(3):534-548.e5.
    doi: 10.1016/j.cmet.2020.01.002.
    IF=22.415(2019)

    PMID: 32004475

    Mol Cell. 2017 Nov 16;68(4):673-685.e6.
    doi: 10.1016/j.molcel.2017.10.022.
    IF=14.548(2019)

    PMID: 29149595

    ACS Nano. 2018 Apr 24;12(4): 3385-3396.
    doi: 10.1021/acsnano.7b08969.
    IF=13.903(2019)

    PMID: 29553709

    Nature Plants. 2016 Dec 22;3: 16206.
    doi: 10.1038/nplants.2016.205.
    IF=13.297(2019)

    PMID: 28005066

    Sci Adv. 2018 Oct 24;4(10): eaat6994.
    doi: 10.1126/sciadv.aat6994.
    IF=12.804(2019)

    PMID: 30417089
    我们的产品现已经出口到下面的研究机构与大学,并且还在增涨
  • Cancer Research Initatives Foundation(CARIF) (Malaysia)
  • University of Medicine and Pharmacy (Romania)
  • Shanghai Institute of Organic Chemistry (China)
  • Macau University of Science and Technology (China)
  • Sri Ramachandra University (India)
  • Shanghai Institute of Biochemistry and Cell Biology (China)
  • Medical University of Gdansk (Poland)
  • Washington State University (USA)
  • Subang Jaya Medical Centre (Malaysia)
  • University of Liège (Belgium)
  • Institute of Chinese Materia Medica (China)
  • Almansora University (Egypt)
  • University of Wollongong (Australia)
  • Seoul National University (Korea)
  • More...
  • 国外学术期刊发表的引用ChemFaces产品的部分文献
  • Dicle Tip Dergisi2020, 47(2),423-430.
  • Int J Anal Chem.2017, 2017:1254721
  • Industrial Crops and Products2023, 199:116746.
  • Int J Mol Sci.2023, 24(8):7045.
  • Biochem Pharmacol.2023, 211:115502.
  • Pharmaceutics.2021, 13(7):1028.
  • Nutrients.2020, 12(12):3638.
  • Biomedicine & Pharmacotherapy2022, 153:113404.
  • University of Manitoba2023, 37433.
  • Int Immunopharmacol. 2020, 83:106403.
  • Int J Mol Sci.2017, 19(1)
  • J Chromatogr B Analyt Technol Biomed Life Sci.2019, 1126-1127:121743
  • Eur J Pharmacol.2021, 906:174220.
  • Processes2021, 9(11),2065.
  • Foods.2022, 11(12):1773.
  • Natural Product Communications2020, doi: 10.1177.
  • Huazhong Agricultural University2022, pp34.
  • Allergol Immunopathol (Madr).2022, 1;50(4):23-30.
  • QASCF2022, 14(4).
  • Molecular Simulation2023, 49(8):799-815.
  • Current Pharmaceutical Analysis2017, 13(5)
  • Molecules.2020, 25(23):5556.
  • Front. Physiol.2022, 790345.
  • ...
  • 生物活性
    Description: Perifosine (KRX-0401, NSC639966) is a novel Akt inhibitor with IC50 of 4.7 μM in MM.1S cells, targets pleckstrin homology domain of Akt. Phase 3.
    Targets: Akt
    In vitro:
    Cytotechnology,2010 Oct;62(5):449-60.
    Perifosine induces cell cycle arrest and apoptosis in human hepatocellular carcinoma cell lines by blockade of Akt phosphorylation.[Pubmed: 20842425]
    Hepatocellular carcinoma (HCC) is one of the most common solid cancers, representing the third cause of cancer-related death among cirrhotic patients. Treatment of advanced HCC has become a very active area of research. Perifosine, a new synthetic alkylphospholipid Akt inhibitor, has shown anti-tumor activity by inhibition of Akt phosphorylation.
    METHODS AND RESULTS:
    In this study, the effect of perifosine on the cell proliferation and apoptosis in hepatoma cells has been investigated. Cell growth inhibition was detected by MTT assay, cell cycle was analyzed by flow cytometry, AnnexinV-FITC apoptosis detection kit was used to detect cell apoptosis, and protein expression was examined by Western blotting analysis. Our present studies showed that Akt phosphorylation was inhibited by perifosine in HepG2 and Bel-7402 human hepatocellular carcinoma cells. Perifosine inhibited the growth of HepG2 cells and Bel-7402 cells in a dose-dependent manner, and arrested cell cycle progression at the G(2) phase. Apoptosis induction became more effective with increasing perifosine concentration. The caspase cascade and its downstream effectors, Poly (ADP-ribose) polymerase (PARP), were also activated simultaneously upon perifosine treatment. The proapoptotic effect of perifosine was in part depending on regulation of the phosphorylation level of ERK and JNK. Perifosine cotreatment substantially increased cytotoxic effects of cisplatin in HepG2 cells. Down-regulating the expression of Bcl-2 and up-regulating the level of Bax may be the potential mechanism for this synergistic effect.
    CONCLUSIONS:
    Our findings suggest that the small molecule Akt inhibitor perifosine shows substantial anti-tumor activity in human hepatoma cancer cell lines, and is a good candidate for treatment combinations with classical cytostatic compounds in hepatocellular carcinoma.
    In vivo:
    Exp Hematol,2007 Jul;35(7):1038-46.
    Alkyl phospholipid perifosine induces myeloid hyperplasia in a murine myeloma model.[Pubmed: 17588472]
    Alkyl-lysophospholipids are a novel class of antitumor agents. Perifosine is a novel alkyl-lysophospholipid that can induce apoptosis in multiple myeloma (MM) tumor cells, both in vitro and in vivo. We investigated the effects of perifosine on the peripheral blood, bone marrow, and spleen of mice inoculated with subcutaneous plasmacytomas.
    METHODS AND RESULTS:
    Immunocompromised mice were inoculated with myeloma cell lines and treated with oral perifosine in either a daily or weekly schedule, or with vehicle only. When plasmacytomas reached 2 cm, mice were sacrificed. Terminal blood was analyzed with a Coulter counter, and counts were confirmed by light microscopy. Marrow and spleen were also analyzed by light microscopy. In control mice, mean hemoglobin was 12 g/dL, white blood cell (WBC) count 7 x 10(9)/L, and mean platelet count was 292 x 10(9)/L. In contrast, the respective values for mice treated with perifosine weekly were 11 g/dL, 9 x 10(9)/L, and 944 x 10(9)/L; and for mice treated with perifosine daily were 10 g/dL, 11 x 10(9)/L, and 752 x 10(9)/L. The increase in WBCs was due, predominantly, to a neutrophilia. Compared to control mice, perifosine treatment induced marrow hypercellularity and splenic white pulp expansion.
    CONCLUSIONS:
    These findings have clinical relevance because myeloid suppression is a dose-limiting toxicity of many cytotoxic agents, and myeloid hyperplasia is usually only observed in the setting of growth factor stimulation. Coupled with its remarkable in vitro MM cytotoxicity, these results strongly support the use of perifosine in clinical trials for patients with MM.
    制备储备液(仅供参考)
    1 mg 5 mg 10 mg 20 mg 25 mg
    1 mM 2.1661 mL 10.8305 mL 21.661 mL 43.3219 mL 54.1524 mL
    5 mM 0.4332 mL 2.1661 mL 4.3322 mL 8.6644 mL 10.8305 mL
    10 mM 0.2166 mL 1.083 mL 2.1661 mL 4.3322 mL 5.4152 mL
    50 mM 0.0433 mL 0.2166 mL 0.4332 mL 0.8664 mL 1.083 mL
    100 mM 0.0217 mL 0.1083 mL 0.2166 mL 0.4332 mL 0.5415 mL
    * Note: If you are in the process of experiment, it's need to make the dilution ratios of the samples. The dilution data of the sheet for your reference. Normally, it's can get a better solubility within lower of Concentrations.
    部分图片展示
    产品名称 产品编号 CAS编号 分子式 = 分子量 位单 联系QQ
    尼艾酚; Nyasol CFN89297 96895-25-9 C17H16O2 = 252.31 5mg QQ客服:2159513211
    6-氨基-3-甲基嘌呤; 3-Methyladenine CFN60037 5142-23-4 C6H7N5 = 149.15 5mg QQ客服:2159513211
    雷公藤宁B; Triptinin B CFN96479 189389-05-7 C20H26O3 = 314.42 5mg QQ客服:1457312923
    R,S-雌马酚; (R,S)-Equol CFN70434 66036-38-2 C15H14O3 = 242.3 5mg QQ客服:215959384

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