Home > DNA/RNA Synthesis & > Gemcitabine HCl

Gemcitabine HCl

盐酸吉西他滨,盐酸吉西他宾,LY188011,LY 188011

Gemcitabine HCl是一种DNA合成抑制剂,作用于PANC1, MIAPaCa2, BxPC3和Capan2细胞时,IC50分别为50 nM, 40 nM, 18 nM和12 nM。

目录号
EY1641
EY1641
EY1641
纯度
99.49%
99.49%
99.49%
规格
50 mg
100 mg
500 mg
原价
350
680
1850
售价
350
680
1850
库存
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Gemcitabine HCl is a DNA synthesis inhibitor. When tested with pancreatic cancer cell line COLO 357 and L3.6pl, Gemcitabine HCl treatment following genistein which sensitized cells to Gemcitabine HCL significantly inhibited cell growth and increased cell apoptosis. In MIA PaCa-2 cells, Gemcitabine HCl showed markedly cytotoxicity to cells with the IC50 value of 49.7 ± 17.7 nM via inhibiting the activity of dDNA.

  • 体外研究

  • 体内研究

    Saline

  • 激酶实验

  • 细胞实验

    0.2 μM

  • 动物实验

    50 mg/kg或100 mg/kg 腹腔注射

  • 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] Shi X, et al. Oncology. 2002, 62(4), 354-362.
    [2] Plunkett, W., et al. 1995. Semin. Oncol. 22: 3-10.
    [3] Heinemann, V., et al. 1992. Cancer Res. 52: 533-539.
    [4] Hui, Y.F., et al. 1997. Am. J. Health Syst. Pharm. 54: 162 -170.
    [5] Mini, E., et al. 2006. Ann. Oncol. 17: 7-12.

    分子式
    C9H11F2N3O4.HCI
    分子量
    299.66
    CAS号
    122111-03-9
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    50 mM
    Water
    100 mM
    Ethanol
    Insoluble

    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
    NCT01678690 Malignant Tumors Drug: Gemcitabine HCl Oral Formulation InnoPharmax Inc. Early Phase 1 2012-08-01 2016-08-31
    NCT01800630 Advanced Solid Malignancies|Malignant Lymphomas Drug: Gemcitabine HCl Oral Formulation InnoPharmax Inc. Phase 1 2013-04-01 2016-08-30
    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
    NCT01272791 Metastatic Pancreatic Cancer Biological: bavituximab|Drug: Gemcitabine Peregrine Pharmaceuticals Phase 2 2011-01-01 2013-05-03
    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
    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
    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
    NCT00808145 Hepatocellular Carcinoma Drug: Gemcitabine / Cisplatin / Sorafenib Lahey Clinic Phase 2 2009-02-01 2014-10-21
    NCT01453153 Stage IV Pancreatic Cancer Drug: Gemcitabine|Drug: PEGPH20+ gemcitabine Halozyme Therapeutics Phase 1|Phase 2 2011-09-01 2015-10-12
    NCT02237157 Pancreatic Cancer Drug: Gemcitabine, local delivery RenovoRx Phase 4 2015-03-01 2016-11-04
    NCT00928642 Ovarian Cancer|Primary Peritoneal Cancer Drug: imatinib mesylate by mouth|Drug: Gemcitabine Intravenous Henry M. Jackson Foundation for the Advancement of Military Medicine|Novartis Phase 2 2009-06-01 2014-10-20
    NCT01051284 Pancreatic Cancer Radiation: Cyberknife radiation and gemcitabine Georgetown University Phase 1 2009-11-01 2012-04-23
    NCT01434459 Pancreatic Neoplasms|Cholangiocarcinoma Drug: Gemcitabine with TheraSphere Emory University Phase 1 2011-09-01 2015-05-01
    NCT01360853 Metastatic Pancreatic Adenocarcinoma Drug: ON 01910.Na|Drug: Gemcitabine|Drug: Gemcitabine Onconova Therapeutics, Inc.|Academic Oncology Gastrointestinal Cancer Consortium (AGICC) Phase 3 2011-05-01 2016-08-02
    NCT00732082 Pancreatic Neoplasms Drug: Gemcitabine|Biological: LAG-3 Washington University School of Medicine Phase 1 2009-02-01 2013-06-11
    NCT00637247 Pancreatic Neoplasms Drug: imexon in combination with gemcitabine|Drug: imexon placebo + gemcitabine AmpliMed Corporation Phase 2 2008-04-01 2010-11-30
    NCT02358161 Pancreatic Cancer Drug: gemcitabine and nab paclitaxel Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA)|Novartis|Celgene Corporation Phase 1|Phase 2 2013-09-01 2015-02-03

    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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