Home > DNA/RNA Synthesis & > Gemcitabine

Gemcitabine

吉西他滨,吉西他宾,LY-188011,NSC-613327

Gemcitabine (吉西他滨; LY-188011; NSC 613327) 是DNA合成抑制剂，对PANC1，MIAPaCa2，BxPC3和Capan2细胞的IC50分别为50 nM，40 nM，18 nM和12 nM。

目录号
EY0987
EY0987
EY0987
纯度
99.57%
99.57%
99.57%
规格
100 mg
200 mg
500 mg
原价
680
990
1500
售价
680
990
1500
库存
现货
现货
现货
订购
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订购
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  • 生物活性

    Gemcitabine is an active chemotherapeutic agents that disrupt DNA replication. In tumor cells, gemcitabine activated checkpoint kinase 2 (Chk2) and ataxia-telangiectasia mutated kinase (ATM), which regulated apoptosis, DNA repair and cell-cycle arrest. Also, gemcitabine activated the Rad9-Hus1-Rad1 complex and the protein kinases ATM and ATR and checkpoint kinase 1 (Chk1), which blocked cell-cycle progression and influence DNA repair. Gemcitabine is a DNA synthesis inhibitor with anti-tumor activity. In human osteosarcoma cell lines HOS and MG63, gemcitabine inhibited DNA synthesis and induced apoptosis.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

  • 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] Hertel LW, et al. Cancer Res, 1990, 50(14), 4417-4422.
    [2] Baker, C.H., et al. 1991. J. Med. Chem. 34: 1879-1884.

    分子式
    C9H11F2N3O4    		 分子量
    263.2    		 CAS号
    95058-81-4     		储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    15 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
    NCT00074607 Meningitis|Neoplasms Drug: Gemcitabine Baylor College of Medicine|Texas Children's Hospital|University of Pittsburgh|National Cancer Institute (NCI)|Children's Hospital of Pittsburg|Seattle Children's Hospital|Mayo Clinic|Brown University Phase 1 2001-12-01 2012-11-09
    NCT01276613 Pancreatic Cancer Drug: Gemcitabine|Drug: Losartan M.D. Anderson Cancer Center 2011-01-01 2016-09-20
    NCT02992015 Diffuse Intrinsic Pontine Glioma Drug: Gemcitabine University of Colorado, Denver|Children's Hospital Colorado Early Phase 1 2016-09-01 2016-12-09
    NCT01938716 Pancreatic Cancer Drug: Gemcitabine M.D. Anderson Cancer Center 2012-03-01 2017-03-02
    NCT02046304 Sarcoma Drug: Gemcitabine|Radiation: Radiation Therapy M.D. Anderson Cancer Center|Eli Lilly and Company Phase 1 2001-12-01 2016-04-04
    NCT00808145 Hepatocellular Carcinoma Drug: Gemcitabine / Cisplatin / Sorafenib Lahey Clinic Phase 2 2009-02-01 2014-10-21
    NCT01869023 Advanced Malignant Pleural Mesothelioma Drug: Gemcitabine|Drug: Cisplatin Instituto Nacional de Cancerologia de Mexico|National Council of Science and Technology, Mexico Phase 2 2010-11-01 2017-03-01
    NCT00620295 Breast Cancer|Colorectal Cancer|Head and Neck Cancer|Kidney Cancer|Lung Cancer|Ovarian Cancer|Pancreatic Cancer|Prostate Cancer|Sarcoma Drug: bortezomib|Drug: gemcitabine hydrochloride Masonic Cancer Center, University of Minnesota Phase 1 2007-03-01 2012-11-06
    NCT01272791 Metastatic Pancreatic Cancer Biological: bavituximab|Drug: Gemcitabine Peregrine Pharmaceuticals Phase 2 2011-01-01 2013-05-03
    NCT01434459 Pancreatic Neoplasms|Cholangiocarcinoma Drug: Gemcitabine with TheraSphere Emory University Phase 1 2011-09-01 2015-05-01
    NCT01453153 Stage IV Pancreatic Cancer Drug: Gemcitabine|Drug: PEGPH20+ gemcitabine Halozyme Therapeutics Phase 1|Phase 2 2011-09-01 2015-10-12
    NCT01051284 Pancreatic Cancer Radiation: Cyberknife radiation and gemcitabine Georgetown University Phase 1 2009-11-01 2012-04-23
    NCT02237157 Pancreatic Cancer Drug: Gemcitabine, local delivery RenovoRx Phase 4 2015-03-01 2016-11-04
    NCT02039518 Small Cell Lung Cancer Drug: gemcitabine|Other: observation group Fudan University Phase 2 2013-12-01 2014-01-15
    NCT00337259 Non-Hodgkin's Lymphoma|Marginal Zone Lymphoma Drug: gemcitabine Asan Medical Center|Eli Lilly and Company Phase 2 2006-06-01 2016-02-13
    NCT00434135 Non-Small Cell Lung Cancer|Stage IIIB or IV Drug: gemcitabine plus pemetrexed, paclitaxel plus gemcitabine Southern Italy Cooperative Oncology Group Phase 2 2006-05-01 2009-02-04
    NCT02030574 Invasive Bladder Cancer|Bladder Cancer Drug: Gemcitabine and fractionated cisplatin (combination treatment) Brown University|Lifespan Phase 2 2014-07-01 2016-07-25
    NCT01171755 Biliary Tract Cancer Drug: Gemcitabine TS-1 Samsung Medical Center Phase 2 2008-02-01 2014-05-20
    NCT00944463 Pancreatic Cancer Drug: Gemcitabine+simvastatin|Drug: Gemcitabine+Placebo Samsung Medical Center Phase 2 2008-10-01 2017-02-15
    NCT00030732 Pancreatic Cancer Drug: Gemcitabine + Capecitabine|Drug: Gemcitabine alone Swiss Group for Clinical Cancer Research|Central European Cooperative Oncology Group Phase 3 2001-06-01 2012-05-14
    NCT01797913 THE Efficacy and Safety of Gemcitabine in the Maintenance Treatment of Advanced Non-small Cell Lung Cancer Drug: gemcitabine Fudan University Phase 2 2008-08-01 2016-02-22
    NCT00375310 Pancreatic Cancer|Adenocarcinoma of the Pancreas Drug: Gemcitabine, Sorafenib|Procedure: Radiotherapy Indiana University School of Medicine|Onyx Pharmaceuticals|Indiana University Phase 1 2006-09-01 2016-02-26

    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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