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Vatalanib 2HCl

二盐酸瓦他拉尼,二盐酸伐他拉尼,ZK 222584,cpg-79787,PTK787 2HCl

Vatalanib (PTK787; ZK-222584; CGP-79787)是VEGFR2/KDR抑制剂，IC50为37 nM，对VEGFR1/Flt-1和VEGFR3/Flt-4抑制性较弱。

目录号
EY1849
EY1849
EY1849
EY1849
纯度
99.33%
99.33%
99.33%
99.33%
规格
5 mg
10 mg
50 mg
100 mg
原价
275
442
1120
1820
售价
275
442
1120
1820
库存
现货
现货
现货
现货
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  • 生物活性

    Vatalanib (PTK787) 2HCl is an oral bioactive, inhibitor of VEGFR2/KDR with IC50 of 37 nM, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4. Vatalanib (PTK787) 2HCl inhibits VEGF-induced autophosphorylation of kinase insert domain-containing receptor (KDR), endothelial cell proliferation, migration, and survival in the nanomolar range in cell-based assays.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    0 - 10 μM

  • 动物实验

    25 mg/kg 到 100 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] Wood JM, et al. Cancer Res. 2000, 60(8), 2178-2189.
    [2] Herbst, R.S., et al. 2007. Expert Opin. Investig. Drugs. 16: 239-249.

    分子式
    C20H17Cl3N4    		 分子量
    419.73    		 CAS号
    212141-51-0    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    30 mg/mL    		 Water
    		 Ethanol
    10 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
    NCT00348790 Brain and Central Nervous System Tumors|Sarcoma Drug: vatalanib Northwestern University|Novartis Phase 2 2006-05-01 2014-10-21
    NCT00072475 Leukemia|Myelodysplastic Syndromes|Myelodysplastic/Myeloproliferative Neoplasms Drug: vatalanib Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI) Phase 2 2003-12-01 2016-07-01
    NCT00590343 Metastatic Neuroendocrine Tumors Drug: vatalanib Louisiana State University Health Sciences Center in New Orleans|Novartis Phase 2 2004-11-01 2011-06-28
    NCT00088231 Acute Myelogenous Leukemia|Agnogenic Myeloid Metaplasia|Chronic Myelogenous Leukemia Drug: Imatinib Mesylate (Gleevec)|Drug: PTK 787 (vatalanib) M.D. Anderson Cancer Center|Novartis Phase 1|Phase 2 2004-07-01 2012-01-19
    NCT00268918 Ovarian Cancer|Endometrial Cancer|Cervical Cancer|Fallopian Tube Cancer|Peritoneal Cancer|Breast Cancer Drug: Docetaxel|Drug: PTK787 Dana-Farber Cancer Institute|Brigham and Women's Hospital|Massachusetts General Hospital Phase 1 2005-09-01 2016-05-05
    NCT00387933 Brain and Central Nervous System Tumors Drug: hydroxyurea|Drug: imatinib mesylate|Drug: vatalanib Duke University|National Cancer Institute (NCI) Phase 1 2005-07-01 2015-10-11
    NCT00056459 Colorectal Neoplasms|Colonic Neoplasms|Rectal Neoplasms Drug: Vatalanib Novartis|Bayer Phase 3 2003-02-01 2009-11-18
    NCT00511043 Lymphoma, Large-Cell, Diffuse Drug: PTK787 David Rizzieri, MD|Novartis Pharmaceuticals|Duke University Phase 2 2005-11-01 2014-11-19
    NCT00056446 Colorectal Neoplasms|Colonic Neoplasms|Rectal Neoplasms Drug: Vatalanib Novartis Pharmaceuticals|Bayer|Novartis Phase 3 2003-01-01 2017-03-02
    NCT00358163 Metastatic Non-hematologic Malignancies Drug: PTK787/ZK 222584|Drug: paclitaxel Massachusetts General Hospital|Novartis Pharmaceuticals|Beth Israel Deaconess Medical Center|Brigham and Women's Hospital|Dana-Farber Cancer Institute Phase 1 2006-04-01 2009-10-30
    NCT00117299 Sarcoma Drug: PTK787/ZK222584 Helsinki University|Bayer Phase 2 2004-09-01 2010-05-25
    NCT00185588 Pancreatic Cancer Drug: Vatalanib|Drug: Gemcitabine George Albert Fisher|Novartis|Stanford University Phase 1|Phase 2 2004-10-01 2014-09-10
    NCT00134355 Prostate Cancer Drug: PTK787 University of Michigan Cancer Center|Novartis Phase 2 2005-07-01 2015-01-15
    NCT00303732 Kidney Cancer|Unspecified Adult Solid Tumor, Protocol Specific Drug: RAD001 (everolimus)|Drug: PTK787 (vatalanib) Daniel George, MD|Novartis|Duke University Phase 1 2004-12-01 2016-03-01
    NCT00226005 Neoplasm Drug: PTK787/ZK222584 Pancreatic Cancer Research Team Phase 2 2005-12-01 2012-05-08
    NCT00731861 Neoplasm Metastasis|Carcinoma Drug: Paclitaxel plus PTK787 Indiana University School of Medicine|Novartis|Indiana University Phase 1 2005-05-01 2014-09-10
    NCT00171587 Tumors|Neoplasm Metastasis Drug: PTK787/ZK 222584 (vatalanib) Novartis|Bayer Phase 1|Phase 2 2002-05-01 2009-11-18
    NCT00627198 Neuroendocrine Tumors Drug: PTK787/ZK222584 - Experimental University of Iowa|Novartis Pharmaceuticals Phase 2 2006-12-01 2010-12-01
    NCT00563823 Melanoma (Skin) Drug: vatalanib Cambridge University Hospitals NHS Foundation Trust|National Cancer Institute (NCI) Phase 2 2006-02-01 2013-08-01
    NCT00053885 Malignant Mesothelioma Drug: PTK787/ZK 222584 Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI) Phase 2 2003-07-01 2016-06-30
    NCT00611793 Refractory Malignancy|Advanced Malignancies Drug: PTK787/ZK222584 and Bevacizumab SCRI Development Innovations, LLC|Novartis Phase 1 2004-10-01 2009-01-22
    NCT00385853 Glioblastoma Drug: PTK787/ZK 222584|Drug: Temozolomide|Procedure: Radiation Therapy Massachusetts General Hospital|Dana-Farber Cancer Institute|Novartis Phase 1 2006-09-01 2013-10-18
    NCT00216047 Breast Cancer Drug: PTK787|Drug: Trastuzumab Hoosier Cancer Research Network|Novartis Pharmaceuticals|Walther Cancer Institute Phase 1|Phase 2 2005-01-01 2015-12-08

    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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