Cediranib 是VEGFR(KDR)高活性抑制剂,IC50为1000倍。
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.
10 μM
5 mg/kg 口服处理
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] 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
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。
相关化合物库
使用AMQUAR产品发表文献后请联系我们