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。
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.
Saline
0.2 μM
50 mg/kg或100 mg/kg 腹腔注射
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] 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
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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