首页 产品中心
  • Bortezomib
  • 保特佐米;Bortezomib;Velcade;MG341;PS-341;PS341;PS 341;LDP-341;MLM341
  • 货号: abs810671
    CAS号: 179324-69-7
    分子式: C19H25BN4O4
    分子量: 384.24
    产品说明书
    分享:
    货号-规格 货期 价格 数量
    abs810671-5mg 现货 ¥482.00
    - +
    abs810671-100mg 现货 ¥2280.00
    - +
    大包装询价
    产品描述
    描述

    Bortezomib is a potent 20S proteasome inhibitor with Ki of 0.6 nM.

    纯度
    >98%
    储存/保存方法
    store at -20℃ for one year(Powder);
    in DMSO or others solvent store at 2-4℃ for two weeks, at -80℃ for six months.
    基本信息
    别名
    保特佐米;Bortezomib;Velcade;MG341;PS-341;PS341;PS 341;LDP-341;MLM341
    外观
    白色至类白色结晶性粉末
    可溶性/溶解性
    DMSO:76 mg/mL (197.79 mM)
    生物活性
    靶点
    20S proteasome
    In vitro(体外研究)
    Bortezomib, a boronic acid dipeptide, is a highly selective, reversible inhibitor of the 26S proteasome which primarily functions in the degradation of mis-folded proteins and is essential for the regulation of the cell cycle. Exposure to Bortezomib has been shown to stabilize p21, p27, and p53, as well as the proapoptotic Bid and Bax proteins, caveolin-1, and inhibitor κB-α, which prevents activation of nuclear factor κB-induced cell survival pathways. Bortezomib also promotes the activation of the proapoptotic c-Jun-NH2 terminal kinase, as well as the endoplasmic reticulum stress response. Alteration of the levels of these cellular proteins leads to inhibition of proliferation, migration, and promotion of apoptosis of cancer cells.Bortezomib is shown to penetrate into cells and inhibit proteasome-mediated intracellular proteolysis of long-lived proteins with a concentration that inhibits 50% of the proteolysis of ∼0.1 μM. The average growth inhibition of 50% value for Bortezomib across the entire panel of 60 cancer cell lines derived from multiple human tumors from the US National Cancer Institute (NCI) is 7 nM. Treatment of PC-3 cells with Bortezomib (100 nM) for 8 h results in the accumulation of cells in G2-M, with a corresponding decrease in the number of cells in G1. Bortezomib kills PC-3 cells at 24 and 48 hr with IC50 of 100 and 20 nM, respectively. Bortezomib induces nuclear condensation at 16–24 hr after treatment. Bortezomib treatment leads to PARP cleavage in a time-dependent manner with concentrations as low as 100 nM being effective at 24 hr.
    In vivo(体内研究)
    The anticancer effects of bortezomib as a single agent have been demonstrated in xenograft models of multiple myeloma, adult T-cell leukemia, lung, breast, prostate, pancreatic, head and neck, and colon cancer, and in melanoma. Oral bortezomib 1.0 mg/ kg daily for 18 days causes tumor growth delays, as well as a decrease in the number of metastases in the Lewis lung cancer model. Bortezomib at a single dose of up to 5 mg/kg significantly decreased the surviving fraction of breast tumor cells. Bortezomib 1.0 mg/kg administrated weekly for 4 weeks reduces tumor growth by 60% in murine xenograft models of prostate cancer. 1.0 mg/kg Bortezomib administration for 4 weeks results in a 72% or 84% reduction in pancreatic cancer murine xenografts growth, as well as an increase in tumor cell apoptosis. 1.0 mg/kg Bortezomib treatment results in significant inhibition of human plasmacytoma xenograft growth, increase in tumor cells apoptosis and overall survival, and a decrease in tumor angiogenesis.
    参考文献
    参考文献
    [1] Adams J, et al. Cancer Res, 1999, 59(11), 2615-2622.
    [2] Boccadoro M, et al. Cancer Cell Int, 2005, 5(1):18.
    [3] LeBlanc R, et al. Cancer Res, 2002, 62(17), 4996-5000
    [4] Stein RL, et al. Biochemistry. 1996, 35(13), 3899-3908.
    [5] Hideshima T, et al. Cancer Res, 2001, 61(7), 3071-3076.
    温馨提示:本产品仅作科研实验使用,不支持临床等研究
        提示: 尊敬的客户您好,如果您对我们的产品有什么疑问或想要了解的,可以点击“我要提问”按钮填写您的疑问。
        提交不成功?请联系info@absin.cn。
        我要提问

    促销资讯 更多

      订购信息
      您可以从我们的授权经销商处购买absin产品或获得技术支持。若要查看您所在地区的经销商,请从以下的下拉列表中选择。
      GO
      • 0