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Vandetanib

凡德他尼,凡他尼布,ZD6474

Vandetanib (凡德他尼; ZD6474)是VEGFR2抑制剂，IC50为40 nM。

目录号
EY1134
EY1134
EY1134
EY1134
纯度
98.94%
98.94%
98.94%
98.94%
规格
1 mg
5 mg
10 mg
100 mg
原价
120
220
400
1800
售价
120
220
400
1800
库存
现货
现货
现货
现货
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  • 生物活性

    Vandetanib is an orally available, potent inhibitor of KDR activity (VEGFR2; IC50 =40 nM), with additional activity versus the tyrosine kinase of the VEGFR3 (IC50 =110 nM) and epidermal growth factor receptor (EGFR/HER1; IC50 =500 nM).

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    0.1–100 μM

  • 动物实验

    12.5 mg/kg/day, 25 mg/kg/day, 50 mg/kg/day, 或 100 mg/kg/day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] Wedge SR, et al. Cancer Res. 2002, 62(16), 4645-4655.
    [2] Bruns, C., et al.: Clin. Cancer Res., 6, 1936 (2000)
    [3] Hennequin, L., et al.: J. Med. Chem., 45, 1300 (2002)
    [4] ark, M., et al.: J. Biol. Chem., 278, 50624 (2003)
    [5] Arao, T., et al.: Cancer Res., 64, 9101 (2004)
    [6] Prueitt, R., et al.: Int. J. Cancer, 120, 796 (2007)

    分子式
    C22H24BrFN4O2    		 分子量
    475.35    		 CAS号
    443913-73-3    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    4 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
    NCT01561781 Healthy Volunteers Drug: Digoxin|Drug: Vandetanib Sanofi Phase 1 2012-03-01 2016-08-26
    NCT01544140 Healthy Volunteers Drug: Midazolam|Drug: vandetanib Sanofi Phase 1 2012-04-01 2016-08-26
    NCT01551615 Healthy Drug: Metformin 1000 mg|Drug: Vandetanib 800 mg Sanofi Phase 1 2012-03-01 2016-08-26
    NCT01661179 Unresectable Locally Advanced or Metastatic, Medullary Thyroid Carcinoma Drug: Vandetanib 300mg Genzyme, a Sanofi Company|Sanofi Phase 1|Phase 2 2012-11-01 2016-10-11
    NCT01823068 Non Small Cell Lung Cancer Drug: Vandetanib Samsung Medical Center|AstraZeneca Phase 2 2013-04-01 2016-04-19
    NCT02109250 All Belgian Patients With Aggressive, Symptomatic Unresectable Locally Advanced or Metastatic Medullary Thyroid Cancer and Taking Caprelsa庐 Will be Included. Drug: Caprelsa Genzyme, a Sanofi Company|Sanofi 2014-04-01 2016-08-30
    NCT00613223 Gliosarcoma|Glioblastoma Drug: Vandetanib and Etoposide Annick Desjardins|AstraZeneca|Duke University Phase 1 2008-02-01 2013-02-19
    NCT01004419 Carcinoma, Non Small Cell Lung Drug: ZD6474 (vandetanib)|Drug: Faslodex (Fulvestrant) University of Wisconsin, Madison|AstraZeneca|University of Pittsburgh Phase 1 2009-11-01 2015-09-30
    NCT00472017 Brain and Central Nervous System Tumors Drug: vandetanib St. Jude Children's Research Hospital Phase 1 2007-04-01 2012-10-11
    NCT01539655 Pharmacokinetic|Cmax|Tmax|Plasma AUC|Plasma [AUC(0-t)]|Plasma [AUC(0-672)]|(t1/2,位z) Drug: vandetanib|Drug: omeprazole|Drug: ranitidine Sanofi Phase 1 2012-02-01 2016-08-26
    NCT01876784 Differentiated Thyroid Cancer Drug: Vandetanib (SAR390530)|Drug: Placebo Genzyme, a Sanofi Company|Sanofi Phase 3 2013-09-01 2017-01-23
    NCT01945762 Symptomatic, Aggressive, Sporadic, Unresectable, Locally|Advanced/Metastatic Medullary Thyroid Cancer (MTC) Drug: Vandetanib 300 mg Genzyme, a Sanofi Company|Worldwide Clinical Trials|Sanofi 2014-02-01 2017-02-28
    NCT01934335 Invasive Breast Cancer Drug: Vandetanib|Other: Placebo Weigel, Ronald|University of Iowa Phase 2 2013-10-01 2017-02-20
    NCT01582191 Advanced Cancers Drug: Vandetanib|Drug: Everolimus M.D. Anderson Cancer Center Phase 1 2012-05-01 2016-08-10
    NCT01298323 Locally Advanced or Metastatic Medullary Thyroid Cancer|Medullary Thyroid Cancer Behavioral: Patient outreach|Drug: Vandetanib Genzyme, a Sanofi Company|Sanofi Phase 3 2011-02-01 2017-01-05
    NCT00441142 Glioblastoma Multiforme|Gliosarcoma Drug: ZD6474|Drug: temozolomide|Radiation: Radiation Therapy Patrick Y. Wen, MD|Dana-Farber Cancer Institute|Beth Israel Deaconess Medical Center|Massachusetts General Hospital|University of Virginia|Memorial Sloan Kettering Cancer Center|Henry Ford Hospital Phase 1|Phase 2 2007-05-01 2016-09-21
    NCT00660725 Advanced Incurable Solid Malignancy Drug: Vandetanib|Drug: Gemcitabine|Drug: Oxaliplatin Leonard Appleman|AstraZeneca|University of Pittsburgh Phase 1 2009-02-01 2014-01-21
    NCT00445549 Ovarian Neoplasms|Fallopian Tube Neoplasms|Peritoneal Neoplasms Drug: Vandetanib National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Phase 2 2007-01-01 2012-05-22
    NCT00923247 Medullary Thyroid Carcinoma Drug: Bortezomib|Drug: Vandetanib National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Phase 1|Phase 2 2009-02-01 2016-11-01
    NCT00821080 Glioblastoma Drug: Sirolimus|Drug: Vandetanib Massachusetts General Hospital|Brigham and Women's Hospital|Dana-Farber Cancer Institute|AstraZeneca Phase 1 2008-10-01 2015-04-30
    NCT01941849 Phaeochromocytoma|Paraganglioma Drug: Vandetanib|Radiation: 131I-mIBG University College, London|Cancer Research UK|AstraZeneca Phase 1 2014-10-01 2015-12-18
    NCT00098345 Thyroid Cancer Drug: ZD6474 (vandetanib) Genzyme, a Sanofi Company|Sanofi Phase 2 2004-11-01 2016-08-24
    NCT02530411 Neoplasms Drug: Fulvestrant|Drug: Vandetanib Velindre NHS Trust|Cancer Research UK|AstraZeneca Phase 2 2015-04-01 2015-08-19

    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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