Home > VEGFR & VEGFR & > Cediranib

Cediranib

西地尼布,NSC-732208,AZD2171,AZD 2171,AZD-2171,NSC 732208,NSC732208,

Cediranib 是VEGFR(KDR)高活性抑制剂,IC50为1000倍。

目录号
EY1586
EY1586
EY1586
EY1586
EY1586
纯度
99.74%
99.74%
99.74%
99.74%
99.74%
规格
1 mg
5 mg
10 mg
50 mg
100 mg
原价
318
699
995
2375
3860
售价
318
699
995
2375
3860
库存
现货
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Cediranib (AZD2171) is a highly potent VEGFR(KDR) inhibitor with IC50 of <1 nM, also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM, similar activity against c-Kit and PDGFRβ, 36-, 110-fold and >1000-fold selective more for VEGFR than PDGFR-α, CSF-1R and Flt3 in HUVEC cells. Phase 3.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    10 μM

  • 动物实验

    5 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 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] Wedge SR, et al. Cancer Res, 2005, 65(10), 4389-4400.

    分子式
    C25H27FN4O3
    分子量
    450.51
    CAS号
    288383-20-0
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    ≥85 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
    NCT00750841 Solid Tumors Drug: cediranib AstraZeneca Phase 1 2008-09-01 2016-09-22
    NCT01262612 Malignant Ascites|Malignant Pleural Effusion Drug: immediate cediranib|Drug: Start cediranib after 28 days Best Supportive Care Radboud University Phase 2 2010-04-01 2013-07-12
    NCT00981721 Advanced Solid Malignancies Drug: cediranib (RECENTIN TM, AZD2171) AstraZeneca Phase 1 2009-09-01 2011-06-17
    NCT00750425 Advanced Solid Tumors Drug: cediranib (RECENTIN TM, AZD2171) AstraZeneca Phase 1 2008-08-01 2011-03-09
    NCT00621725 Advanced Cancer|Hepatic Impairment Drug: AZD2171 AstraZeneca Phase 1 2008-01-01 2014-07-14
    NCT00503204 Recurrent Glioblastoma|Brain Tumor Drug: Cediranib|Drug: Lomustine AstraZeneca Phase 1 2007-09-01 2009-11-24
    NCT00532194 Ovarian Cancer Drug: cediranib Medical Research Council|Cancer Research UK|National Health and Medical Research Council, Australia|ANZGOG|NCIC Clinical Trials Group|Grupo Espaol de Investigacin en Cncer de Ovario|AstraZeneca Phase 3 2007-07-01 2015-09-21
    NCT00306891 Cancer Drug: Cediranib|Drug: Cediranib 30 - 90 mg AstraZeneca Phase 2 2006-06-01 2012-10-03
    NCT00979862 Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Recurrent Adult Brain Neoplasm Drug: Cediranib Maleate|Drug: Cilengitide|Other: Laboratory Biomarker Analysis National Cancer Institute (NCI) Phase 1 2010-03-01 2015-04-14
    NCT01337401 Alveolar Soft-part Sarcoma Drug: Cediranib|Drug: Placebo Institute of Cancer Research, United Kingdom|Royal Marsden NHS Foundation Trust Phase 2 2011-05-01 2016-08-02
    NCT01391962 Sarcoma, Alveolar Soft Part Drug: Cediranib|Drug: Sunitinib National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Phase 2 2011-06-17 2017-03-10
    NCT00423332 Renal Cell Carcinoma Drug: Cediranib|Drug: Cediranib Placebo AstraZeneca Phase 2 2007-01-01 2016-12-08
    NCT01132820 Endometrial Adenocarcinoma|Endometrial Adenosquamous Carcinoma|Endometrial Clear Cell Adenocarcinoma|Endometrial Serous Adenocarcinoma|Recurrent Uterine Corpus Carcinoma Drug: Cediranib Maleate|Other: Laboratory Biomarker Analysis National Cancer Institute (NCI) Phase 2 2010-06-01 2016-04-20
    NCT00458731 Adult Grade III Lymphomatoid Granulomatosis|Adult Nasal Type Extranodal NK/T-cell Lymphoma|Anaplastic Large Cell Lymphoma|Angioimmunoblastic T-cell Lymphoma|Childhood Burkitt Lymphoma|Childhood Diffuse Large Cell Lymphoma|Childhood Grade III Lymphomatoid Granulomatosis|Childhood Immunoblastic Large Cell Lymphoma|Childhood Nasal Type Extranodal NK/T-cell Lymphoma|Cutaneous B-cell Non-Hodgkin Lymphoma|Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue|Hepatosplenic T-cell Lymphoma|Intraocular Lymphoma|Nodal Marginal Zone B-cell Lymphoma|Noncutaneous Extranodal Lymphoma|Peripheral T-cell Lymphoma|Progressive Hairy Cell Leukemia, Initial Treatment|Recurrent Adult Burkitt Lymphoma|Recurrent Adult Diffuse Large Cell Lymphoma|Recurrent Adult Diffuse Mixed Cell Lymphoma|Recurrent Adult Diffuse Small Cleaved Cell Lymphoma|Recurrent Adult Hodgkin Lymphoma|Recurrent Adult Immunoblastic Large Cell Lymphoma|Recurrent Adult Lymphoblastic Lymphoma|Recurrent Adult T-cell Leukemia/Lymphoma|Recurrent Childhood Anaplastic Large Cell Lymphoma|Recurrent Childhood Large Cell Lymphoma|Recurrent Childhood Lymphoblastic Lymphoma|Recurrent Childhood Small Noncleaved Cell Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Mycosis Fungoides/Sezary Syndrome|Recurrent/Refractory Childhood Hodgkin Lymphoma|Refractory Hairy Cell Leukemia|Small Intestine Lymphoma|Splenic Marginal Zone Lymphoma|Stage IV Adult Burkitt Lymphoma|Stage IV Adult Diffuse Large Cell Lymphoma|Stage IV Adult Diffuse Mixed Cell Lymphoma|Stage IV Adult Diffuse Small Cleaved Cell Lymphoma|Stage IV Adult Hodgkin Lymphoma|Stage IV Adult Immunoblastic Large Cell Lymphoma|Stage IV Adult Lymphoblastic Lymphoma|Stage IV Adult T-cell Leukemia/Lymphoma|Stage IV Childhood Anaplastic Large Cell Lymphoma|Stage IV Childhood Hodgkin Lymphoma|Stage IV Childhood Large Cell Lymphoma|Stage IV Childhood Lymphoblastic Lymphoma|Stage IV Childhood Small Noncleaved Cell Lymphoma|Stage IV Grade 1 Follicular Lymphoma|Stage IV Grade 2 Follicular Lymphoma|Stage IV Grade 3 Follicular Lymphoma|Stage IV Mantle Cell Lymphoma|Stage IVA Mycosis Fungoides/Sezary Syndrome|Stage IVB Mycosis Fungoides/Sezary Syndrome|T-cell Large Granular Lymphocyte Leukemia|Testicular Lymphoma|Unspecified Adult Solid Tumor, Protocol Specific|Unspecified Childhood Solid Tumor, Protocol Specific|Waldenstrm Macroglobulinemia Biological: bevacizumab|Drug: cediranib maleate National Cancer Institute (NCI) Phase 1 2007-05-01 2014-02-14
    NCT02340611 Ovarian Cancer Drug: Olaparib|Drug: Cediranib University Health Network, Toronto|AstraZeneca Phase 2 2015-06-01 2016-06-21
    NCT00278343 Recurrent Fallopian Tube Cancer|Recurrent Ovarian Epithelial Cancer|Recurrent Primary Peritoneal Cavity Cancer Drug: cediranib maleate|Other: laboratory biomarker analysis National Cancer Institute (NCI) Phase 2 2006-04-01 2014-08-05
    NCT00264004 Tumors Drug: AZD2171 AstraZeneca Phase 2 2005-11-01 2012-07-26
    NCT00494221 Metastatic Colorectal Cancer Drug: AZD2171|Drug: FOLFOX (5-fluorouracil, Leucovorin, Oxaliplatin)|Drug: Placebo Cediranib AstraZeneca Phase 1|Phase 2 2007-06-01 2014-02-26
    NCT01116648 Estrogen Receptor Negative|HER2/Neu Negative|Ovarian Endometrioid Adenocarcinoma|Ovarian Serous Cystadenocarcinoma|Ovarian Serous Surface Papillary Adenocarcinoma|Progesterone Receptor Negative|Recurrent Breast Carcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Triple-Negative Breast Carcinoma Drug: Cediranib Maleate|Other: Laboratory Biomarker Analysis|Drug: Olaparib|Other: Pharmacological Study National Cancer Institute (NCI) Phase 1|Phase 2 2010-03-01 2017-01-31
    NCT00238394 Adult Primary Hepatocellular Carcinoma|Advanced Adult Primary Liver Cancer|Localized Unresectable Adult Primary Liver Cancer Drug: cediranib maleate|Other: laboratory biomarker analysis National Cancer Institute (NCI) Phase 2 2005-12-01 2013-06-04
    NCT01229111 Adult Primary Cholangiocellular Carcinoma|Advanced Adult Primary Liver Cancer|Cholangiocarcinoma of the Extrahepatic Bile Duct|Cholangiocarcinoma of the Gallbladder|Localized Unresectable Adult Primary Liver Cancer|Periampullary Adenocarcinoma|Recurrent Adult Primary Liver Cancer|Recurrent Extrahepatic Bile Duct Cancer|Recurrent Gallbladder Cancer|Unresectable Extrahepatic Bile Duct Cancer|Unresectable Gallbladder Cancer Drug: cediranib maleate|Drug: oxaliplatin|Drug: leucovorin calcium|Drug: fluorouracil National Cancer Institute (NCI) Phase 2 2010-10-01 2016-09-19
    NCT00937482 Male Breast Cancer|Stage IV Breast Cancer|Stage IV Melanoma|Stage IV Non-small Cell Lung Cancer|Stage IV Renal Cell Cancer|Stage IVA Colon Cancer|Stage IVA Rectal Cancer|Stage IVB Colon Cancer|Stage IVB Rectal Cancer|Tumors Metastatic to Brain Drug: cediranib maleate|Radiation: whole-brain radiation therapy National Cancer Institute (NCI) Phase 1 2009-08-01 2013-03-07
    NCT00309946 Advanced Malignant Mesothelioma|Epithelial Mesothelioma|Localized Malignant Mesothelioma|Recurrent Malignant Mesothelioma|Sarcomatous Mesothelioma Drug: cediranib maleate National Cancer Institute (NCI) Phase 2 2005-12-01 2014-07-25
    NCT00475956 Neoplasms Drug: AZD2171|Drug: AZD0530 AstraZeneca Phase 1 2007-05-01 2010-04-14
    NCT01131234 Adult Anaplastic Astrocytoma|Adult Anaplastic Ependymoma|Adult Anaplastic Oligodendroglioma|Adult Brain Stem Glioma|Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Adult Mixed Glioma|Adult Solid Neoplasm|Male Breast Carcinoma|Recurrent Adult Brain Neoplasm|Recurrent Breast Carcinoma|Recurrent Colon Carcinoma|Recurrent Melanoma|Recurrent Non-Small Cell Lung Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Ovarian Germ Cell Tumor|Recurrent Pancreatic Carcinoma|Recurrent Rectal Carcinoma|Recurrent Renal Cell Carcinoma|Stage III Pancreatic Cancer|Stage III Renal Cell Cancer|Stage IIIA Colon Cancer|Stage IIIA Non-Small Cell Lung Cancer|Stage IIIA Ovarian Cancer|Stage IIIA Ovarian Germ Cell Tumor|Stage IIIA Rectal Cancer|Stage IIIA Skin Melanoma|Stage IIIB Breast Cancer|Stage IIIB Colon Cancer|Stage IIIB Non-Small Cell Lung Cancer|Stage IIIB Ovarian Cancer|Stage IIIB Ovarian Germ Cell Tumor|Stage IIIB Rectal Cancer|Stage IIIB Skin Melanoma|Stage IIIC Breast Cancer|Stage IIIC Colon Cancer|Stage IIIC Ovarian Cancer|Stage IIIC Ovarian Germ Cell Tumor|Stage IIIC Rectal Cancer|Stage IIIC Skin Melanoma|Stage IV Breast Cancer|Stage IV Non-Small Cell Lung Cancer|Stage IV Ovarian Cancer|Stage IV Ovarian Germ Cell Tumor|Stage IV Pancreatic Cancer|Stage IV Renal Cell Cancer|Stage IV Skin Melanoma|Stage IVA Colon Cancer|Stage IVA Rectal Cancer|Stage IVB Colon Cancer|Stage IVB Rectal Cancer Drug: Gamma-Secretase Inhibitor RO4929097|Drug: Cediranib Maleate|Other: Pharmacological Study|Other: Laboratory Biomarker Analysis National Cancer Institute (NCI) Phase 1 2010-05-01 2014-12-22

    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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