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Etoposide

依托泊苷,依托泊甙,足叶乙苷,依托扑沙,鬼臼乙叉甙,依托泊甘,VP-16,VP-16213

Etoposide是鬼臼毒素的一种半合成衍生物，通过抑制拓扑异构酶II活性而抑制DNA合成。

目录号
EY1451
EY1451
EY1451
纯度
99.71%
99.71%
99.71%
规格
100 mg
200 mg
500 mg
原价
400
700.00_
1,480.00_
售价
400
700.00_
1,480.00_
库存
现货
现货
现货
订购
订购
订购
订购
订购
订购
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  • 生物活性

    The activity of the topoisomerase II enzyme on re-ligation of DNA strands is interrupted by etoposide. A ternary complex with DNA is formed by etoposide, and causes DNA strands to break. The enzyme was more important in cancer cell than healthy cells, because cancer cells divided more rapidly. So etoposide induced apoptosis of the cancer cells. Etoposide exhibited cytotoxic activity against HepG2 and MOLT-3 cancer cells with IC50 of 30.16 μM and 0.051μM. The IC50 values of etoposide against the tumor cell lines of BGC-823, HeLa, and A549 were 43.74 ± 5.13, 209.90 ± 13.42, and 139.54 ± 7.05 μM, respectively.

  • 体外研究

  • 体内研究

    30% Propylene glycol, 5% Tween 80, 65% D5W(5%葡萄糖水溶液)

  • 激酶实验

  • 细胞实验

    80 μg/mL

  • 动物实验

    10 mg/kg 从实验第7天开始，每天腹腔注射，持续5天

  • 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 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。

  • 参考文献

    [1] van Maanen JM et al, J Natl Cancer Inst, 1988, 80(19), 1526-1533.
    [2] Terada et al (1993) Antitumor agents.3.Synthesis and biological activity of 4β-alkyl derivatives containing hydroxy, amino, and amido groups of 4'-O-demethyl-4-desoxypodophyllotoxin as antitumor agents. J.Med.Chem. 36 1689.
    [3] Hainsworth, J.D. and Greco, F.A. 1995. Ann. Oncol. 6: 325-341.
    [4] Burden et al (1996) Toposiomerase II.etoposide interactions direct the formation of drug-induced enzyme-DNA cleavage complexes. J.Biol.Chem. 271 29238.
    [5] Fearnhead, H.O., et al. 1994. Biochem. Pharmacol. 48: 1073-1079.
    [6] Hande et al (1998) Etoposide: four decades of development of a topoisomerase II inhibitor. Eur.J.Cancer 34 1514.

    分子式
    C29H32O13    		 分子量
    588.56    		 CAS号
    33419-42-0    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    100 mM    		 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
    NCT01064466 Small Cell Lung Cancer Drug: ETOPOSIDE - Usual|Drug: ETOPOSIDE - Study Dr. Han Xu, President/CEO / PD / PI / Monitor / IRB Chair|Medicine Invention Design, Inc Phase 3 2016-08-01 2017-03-02
    NCT00613223 Gliosarcoma|Glioblastoma Drug: Vandetanib and Etoposide Annick Desjardins|AstraZeneca|Duke University Phase 1 2008-02-01 2013-02-19
    NCT01492556 Breast Cancer Drug: Etoposide Chinese Academy of Medical Sciences|Beijing Cancer Hospital|Peking Union Medical College Hospital|Beijing Chao Yang Hospital|China-Japan Friendship Hospital|Beijing Hospital of the Ministry of Health|The First Affiliated Hospital of Dalian Medical University|Harbin Medical University|Zhejiang Cancer Hospital|Henan Cancer Hospital|Guangxi Cancer Hospital|Shanghai Putuo District Center Hospital|International Peace Maternity and Child Health Hospital|Xinjiang Medical University Phase 2 2011-12-01 2013-03-14
    NCT02733107 Non-small Cell Lung Cancer Drug: Apatinib|Drug: Etoposide Third Military Medical University Phase 2 2016-03-01 2016-04-10
    NCT00612430 Glioblastoma|Gliosarcoma Drug: Bevacizumab and Etoposide Duke University|Genentech, Inc. Phase 2 2007-03-01 2013-07-30
    NCT00702962 Small Cell Lung Cancer Drug: Vorinostat, Carboplatin, Etoposide|Other: SAHA Milton S. Hershey Medical Center|Merck Sharp & Dohme Corp. Phase 1|Phase 2 2008-09-01 2017-01-26
    NCT02773732 Leukemia|Acute Myelogenous Leukemia|Acute Myeloid Leukemia Drug: Ciprofloxacin|Drug: Etoposide University of Florida Phase 1|Phase 2 2016-09-01 2016-09-22
    NCT02867956 Ovarian Cancer Drug: Apatinib|Drug: Etoposide Sun Yat-sen University Phase 2 2016-08-01 2016-08-13
    NCT00504140 Osteosarcoma Drug: Etoposide|Drug: Interferon Alpha M.D. Anderson Cancer Center|Schering-Plough Phase 2 1996-11-01 2012-08-01
    NCT00002880 Lymphoma Drug: Etoposide phosphate Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI) Phase 2 1996-11-01 2016-06-27
    NCT00176605 Prostate Cancer Drug: Etoposide|Drug: Cyclophosphamide Rutgers, The State University of New Jersey|National Cancer Institute (NCI)|Bristol-Myers Squibb Phase 2 2005-05-01 2014-04-18
    NCT00958022 Small Cell Lung Cancer Drug: LBH589 and carboplatin with etoposide Ahmad Tarhini|Novartis Pharmaceuticals|University of Pittsburgh Phase 1 2009-09-01 2016-01-04
    NCT00810017 HER-2 Positive Metastatic Breast Cancer Drug: Etoposide|Drug: Trastuzumab Washington Hospital Center|Genentech, Inc. Phase 2 2009-02-01 2011-11-04
    NCT00544596 Extensive Stage Small Cell Lung Cancer|Unspecified Adult Solid Tumor, Protocol Specific Drug: R-(-)-gossypol acetic acid|Drug: cisplatin|Drug: etoposide National Cancer Institute (NCI) Phase 1 2007-09-01 2014-04-01
    NCT01294670 Solid Tumors|Relapsed/Refractory Sarcomas Drug: Vorinostat and Etoposide Memorial Sloan Kettering Cancer Center|Merck Sharp & Dohme Corp.|Phoenix Children's Hospital|Milton S. Hershey Medical Center|Johns Hopkins University|Sidney Kimmel Comprehensive Cancer Center|Children's Hospital Colorado|University of Florida|Alberta Children's Hospital|M.D. Anderson Cancer Center|Dana-Farber Cancer Institute|Children's Mercy Hospital & Clinics|Johns Hopkins All Children's Hospital|Arnold Palmer Hospital for Children Phase 1|Phase 2 2011-02-01 2017-03-01
    NCT00667615 Hodgkin's Disease|Lymphoma Drug: rituximab, cyclophosphamide, etoposide, prednisone, vorinostat and QOL questionnaire, peg-filgrastim or filgrastim Memorial Sloan Kettering Cancer Center|Merck Sharp & Dohme Corp.|Northwestern University|NorthShore University HealthSystem Research Institute|Weill Medical College of Cornell University Phase 1|Phase 2 2008-04-01 2017-02-22
    NCT00513162 Neuroectodermal Tumor|Brain Metastases|Advanced Cancer Drug: Valproate|Drug: Etoposide M.D. Anderson Cancer Center Phase 1 2007-07-01 2012-09-18
    NCT01084759 Prostate Cancer Drug: Testosterone injection|Drug: Etoposide Sidney Kimmel Comprehensive Cancer Center 2010-03-01 2016-04-05
    NCT02194049 Extensive Stage Small Cell Lung Cancer|Unspecified Adult Solid Tumor, Protocol Specific Drug: BKM120|Drug: cisplatin|Drug: etoposide University of California, Davis|Novartis Phase 1 2014-07-01 2016-06-20
    NCT00856830 Small Cell Lung Cancer|Extensive Stage Lung Cancer|Chemonaive Drug: Bendamustine, Irinotecan, Etoposide/Carboplatin (Novel drug combination) University of Alabama at Birmingham|National Comprehensive Cancer Network Phase 1|Phase 2 2009-03-01 2016-07-07

    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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