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Cisplatin

顺铂,lederplatin

Cisplatin是一种无机的水溶性的铂配合物,通过形成DNA交联剂而抑制DNA合成。

目录号
EY0024
EY0024
纯度
99.12%
99.12%
规格
10 mg
100 mg
原价
100
280
售价
100
280
库存
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Cisplatin is an anticancer agent with some side effects. It is believed to induce apoptosis through several mechanisms. The traditional mechanism is that cisplatin enters the cell, interacts with the DNA guanine bases and forms the inter- or intra-strand chain cross-linking, then prevents the replication of DNA. This formation can also induce apoptosis by activating p53. Cisplatin was also found to cause ROS generation and increase lipid peroxidation, which leads cells to the apoptotic pathway. In addition, cisplatin induces apoptosis with the caspase-dependent pathway. In cochlear cells, cisplatin treatment results in the increase of caspases-3 and -9 and causes the cochlear damage side effect.

  • 体外研究

  • 体内研究

    0.9% NaCl 溶液

  • 激酶实验

  • 细胞实验

    7 μg/mL

  • 动物实验

    5 mg/kg 实验开始第0天和第7天静脉注射

  • 不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 AKm系数


    例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。


  • 参考文献

    [1] Siddik, Z.H., Cisplatin: mode of cytotoxic action and molecular basis of resistance. Oncogene, 2003. 22(47): p. 7265-79.
    [2] Wang, X., J.L. Martindale, and N.J. Holbrook, Requirement for ERK activation in cisplatin-induced apoptosis. J Biol Chem, 2000. 275(50): p. 39435-43.
    [3] Cummings, B.S. and R.G. Schnellmann, Cisplatin-induced renal cell apoptosis: caspase 3-dependent and -independent pathways. J Pharmacol Exp Ther, 2002. 302(1): p. 8-17.
    [4] Lieberthal, W., V. Triaca, and J. Levine, Mechanisms of death induced by cisplatin in proximal tubular epithelial cells: apoptosis vs. necrosis. Am J Physiol, 1996. 270(4 Pt 2): p. F700-8.
    [5] Lieberthal, W., V. Triaca, and J. Levine, Mechanisms of death induced by cisplatin in proximal tubular epithelial cells: apoptosis vs. necrosis. Am J Physiol, 1996. 270(4 Pt 2): p. F700-8.

    分子式
    Cl2H6N2Pt
    分子量
    300.05
    CAS号
    15663-27-1
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    25 mg/mL
    Water
    <1 mg/mL
    Ethanol
    <1 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT01611727 BRCA1 Mutation|Metastatic Breast Cancer Drug: Cisplatin Pomeranian Medical University Szczecin|Maria Sklodowska-Curie Memorial Cancer Center, Institute of Oncology Phase 2 2007-07-01 2012-07-10
    NCT00916500 CERVICAL NEOPLASMS Drug: CONCURRENT CHEMORADIATION (CISPLATIN) Korea Cancer Center Hospital Phase 2 2006-03-01 2014-04-29
    NCT00901537 Non-small Cell Lung Cancer|Squamous Cell Carcinoma of the Head and Neck Drug: Azacitidine and Cisplatin Loma Linda University Phase 1 2009-02-01 2014-06-02
    NCT01561586 Cervical Cancer Drug: Weekly cisplatin with RT|Drug: Tri-weekly cisplatin with RT Korea Cancer Center Hospital|Seoul National University Hospital|Asan Medical Center|Gangnam Severance Hospital Phase 3 2012-03-01 2016-02-24
    NCT01149798 Metastatic Breast Cancer Drug: Abraxane and Cisplatin combination Fudan University Phase 2 2010-06-01 2012-08-05
    NCT00935961 HEAD & NECK Cancer Drug: RAD001 + docetaxel + cisplatin Memorial Sloan Kettering Cancer Center|Novartis Pharmaceuticals Phase 1 2009-07-01 2013-08-07
    NCT00353015 Gastrointestinal Cancer|Carcinoma, Neuroendocrine Drug: Cisplatin|Drug: Irinotecan M.D. Anderson Cancer Center|Pharmacia Phase 2 2003-03-01 2012-08-01
    NCT00808145 Hepatocellular Carcinoma Drug: Gemcitabine / Cisplatin / Sorafenib Lahey Clinic Phase 2 2009-02-01 2014-10-21
    NCT00995761 Non-small Cell Lung Cancer Drug: Docetaxel and Cisplatin Gyeongsang National University Hospital Phase 2 2009-10-01 2014-02-09
    NCT01096745 Metastatic Biliary Tract Cancer|Locally Advanced Biliary Tract Cancer Drug: Gemcitabine, Cisplatin|Drug: S-1, Cisplatin Gyeongsang National University Hospital|Samsung Medical Center|Dong-A University|Chung-Ang University Phase 2 2010-07-01 2011-06-21
    NCT02030574 Invasive Bladder Cancer|Bladder Cancer Drug: Gemcitabine and fractionated cisplatin (combination treatment) Brown University|Lifespan Phase 2 2014-07-01 2016-07-25
    NCT01165385 Solid Tumors|Metastatic Cancer Drug: cisplatin|Drug: Pazopanib UNICANCER Phase 1 2010-06-01 2014-11-14
    NCT00998036 Triple Negative Breast Cancer Drug: Temsirolimus, cisplatin, erlotinib Columbia University|Wyeth is now a wholly owned subsidiary of Pfizer|Genentech, Inc. Phase 1 2009-09-01 2016-02-03
    NCT01114958 Lung Neoplasms|Neoplasm Metastasis Drug: Cisplatin, Thiosulfate University of California, San Diego Phase 1 2010-04-01 2010-05-04
    NCT01336842 Solid Tumors|Non-Small Cell Lung Cancer (NSCLC) Drug: Panobinostat, Cisplatin, Pemetrexed University of California, Davis|Novartis Pharmaceuticals Phase 1 2011-04-01 2017-01-19
    NCT00968435 Head and Neck Cancer Other: bevacizumab, cisplatin, cetuximab, radiation therapy Memorial Sloan Kettering Cancer Center|Genentech, Inc. Phase 2 2009-08-01 2016-08-09

    注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。

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