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Sorafenib Tosylate

甲苯磺酸索拉非尼,甲苯磺酸索拉菲尼,Bay 43-9006

Sorafenib Tosylate是酪氨酸激酶(VEGFR和PDGFR)和RAF/MEK/ERK级联抑制剂，同时作用于Raf-1，wtBRAF和V599EBRAF，IC50分别为6 nM， 22 nM和38 nM。

目录号
EY1396
EY1396
EY1396
EY1396
纯度
99.44%
99.44%
99.44%
99.44%
规格
5 mg
10 mg
50 mg
100 mg
原价
150
300
600
820
售价
150
300
600
820
库存
现货
现货
现货
现货
订购
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  • 生物活性

    Sorafenib tosylate, also named nexavar, is a small-molecule anticancer compound. It is also a novel oral Raf kinase and a vascular endothelial growth factor receptor (VEGFR) inhibitor. It inhibits tumor cell proliferation and tumor angiogenesis. To HepG2 cells (106), the IC50 of sorafenib tosylate is 2.09μg/ml.

  • 体外研究

  • 体内研究

    2% Cremophor EL, 2% N,N-dimethylacetamide

  • 激酶实验

  • 细胞实验

    0 μM -10 μM

  • 动物实验

    30 mg/kg或60 mg/kg 口服处理

  • 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] Wilhelm SM, et al. Cancer Res, 2004, 64(19), 7099-7109.

    分子式
    C21H16ClF3N4O3.C7H8O3S    		 分子量
    637.03    		 CAS号
    475207-59-1    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    127 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
    NCT02122003 Metastatic Renal Cell Carcinoma Drug: Sorafenib Fondazione IRCCS Istituto Nazionale dei Tumori, Milano Phase 2 2014-05-01 2014-04-22
    NCT00478114 Renal Cell Carcinoma Drug: sorafenib Mahidol University|Bayer Phase 3 2007-05-01 2011-08-25
    NCT02636426 Neoplasms Drug: sorafenib VU University Medical Center Phase 1 2015-09-01 2017-03-17
    NCT01425216 Keloids Drug: Sorafenib Tirgan, Michael H., M.D. Phase 2 2013-03-01 2016-10-17
    NCT00390325 Multiple Endocrine Neoplasia|Recurrent Thyroid Gland Carcinoma|Thyroid Gland Medullary Carcinoma Other: Laboratory Biomarker Analysis|Other: Pharmacological Study|Drug: Sorafenib Tosylate National Cancer Institute (NCI) Phase 2 2006-10-01 2017-02-14
    NCT02288507 Hepatocellular Cancer Drug: Sorafenib|Radiation: yttrium-90 radioembolization University of Hawaii Phase 1 2014-11-01 2014-11-10
    NCT00480389 Renal Cell Carcinoma|Metastatic Disease Drug: Sorafenib University Health Network, Toronto|Bayer Phase 2 2007-05-01 2015-12-07
    NCT00997022 Hepatocellular Cancer Drug: Sorafenib Columbia University|Bayer|Onyx Pharmaceuticals Phase 1 2009-05-01 2015-08-07
    NCT00780169 Metastatic Colorectal Cancer Drug: sorafenib + FOLFIRI Ottawa Hospital Research Institute|Bayer Phase 1 2008-10-01 2013-05-09
    NCT02084732 Thyroid Cancer Drug: Sorafenib Instituto Nacional de Cancerologia, Columbia Phase 2 2013-10-01 2016-08-16
    NCT00544609 Bladder Cancer Drug: Sorafenib|Procedure: Radiotherapy Spanish Oncology Genito-Urinary Group Phase 1 2007-12-01 2014-10-01
    NCT00093613 Adult Anaplastic Astrocytoma|Adult Anaplastic Oligodendroglioma|Adult Giant Cell Glioblastoma|Adult Gliosarcoma|Recurrent Adult Brain Tumor Drug: sorafenib tosylate|Other: pharmacological study National Cancer Institute (NCI) Phase 1 2004-12-01 2014-05-29
    NCT02733809 Hepatocellular Carcinoma Drug: Sorafenib King Saud University|King Faisal Specialist Hospital & Research Center Phase 4 2014-01-01 2016-04-05
    NCT00767468 Liver Cancer Drug: sorafenib tosylate UNC Lineberger Comprehensive Cancer Center|National Cancer Institute (NCI) Phase 1 2008-10-01 2012-05-22
    NCT02021929 Hepatopulmonary Syndrome Drug: Sorafenib|Drug: Placebo University of Pennsylvania|National Heart, Lung, and Blood Institute (NHLBI) Phase 2 2014-03-01 2016-07-05
    NCT00933777 Unspecified Adult Solid Tumor, Protocol Specific|Non-Small Cell Lung Cancer Drug: Combination of sorafenib and everolimus University of Cologne Phase 1 2009-07-01 2016-05-24
    NCT01303341 Adult Solid Neoplasm|Recurrent Melanoma|Stage IIIA Skin Melanoma|Stage IIIB Skin Melanoma|Stage IIIC Skin Melanoma Other: Laboratory Biomarker Analysis|Other: Pharmacological Study|Drug: Riluzole|Drug: Sorafenib Tosylate National Cancer Institute (NCI) Phase 1 2011-02-01 2017-02-06
    NCT01510756 Chronic Lymphocytic Leukemia Drug: Sorafenib Thomas Kipps|Bayer|University of California, San Diego Phase 2 2011-12-01 2015-12-16
    NCT00875745 Leukemia, Myeloid, Acute|Leukemia, Promyelocytic, Acute|Myelodysplastic Syndromes Drug: Sorafenib-Vorinostat Indiana University School of Medicine|Bayer|Indiana University Phase 1 2009-04-01 2014-09-17
    NCT01203787 Hepatocellular Carcinoma Drug: Sorafenib Standard Dosing Regimen|Drug: Sorafenib Ramp-Up Regimen University of Florida Phase 4 2010-12-01 2015-02-13
    NCT00954278 Carcinoma, Non Small Cell Lung Drug: sorafenib University of Wisconsin, Madison|Bayer Phase 1 2009-07-01 2016-11-28
    NCT01005199 Liver Cancer Drug: everolimus|Drug: sorafenib tosylate Swiss Group for Clinical Cancer Research Phase 2 2009-11-01 2016-04-14
    NCT01342627 Metastatic Renal Cell Carcinoma Drug: Sorafenib Centro di Riferimento Oncologico - Aviano Phase 2 2010-10-01 2015-10-05

    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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