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。
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.
0.9% NaCl 溶液
7 μg/mL
5 mg/kg 实验开始第0天和第7天静脉注射
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km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。
[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
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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