Catalog No.S1017 Synonyms: NSC-732208
Molecular Weight(MW): 450.51
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.
Cited by 17 Publications
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Western blots of EZH2 expression in A549, HCC461, and HCC4006 cells upon treatment with different doses of VEGFR-2-inhibitor AZD2171 (0, 5 and 10 nM). AZD2171 decreased the expression of EZH2 in HCC4006 and HCC461 cells expressing VEGFR-2 in a dose-dependent manner but did not do so in A549 cells lacking expression of VEGFR-2.
Clin Cancer Res 2014 20, 3849-61. Cediranib (AZD2171) purchased from Selleck.
Representative histological tumor sections with CD31 vascular staining (brown) and hematoxylin nuclear counterstain (blue) from the 4 treatment groups(untreated, quinacrine, cediranib, ced+quin). Discrete staining is associated with vascular endothelial cells, whereas more diffuse and variable staining is nonspecific and associated with tumor necrosis. Microvessel examples are marked by arrows.
Neuro Oncol 2013 15, 1673-83. Cediranib (AZD2171) purchased from Selleck.
(A) Representative LC3 Western blots obtained from 4C8 cells grown under normoxic (20% O2) or hypoxic (0.5% O2) conditions for 10 h while untreated or exposed to cediranib (3 uM), quinacrine (0.8 uM), or combined cediranib/quinacrine. (B) RFP-LC3-expressing 4C8 cells were visualized using EVOS fl microscopy, grown under hypoxic conditions for 24 h while untreated or exposed to cediranib (2.5 uM), quinacrine (2.5 uM), or combined cediranib/quinacrine. (C) Representative cleaved caspase-3 Western blots obtained from 4C8 cells grown under normoxic (20% O2) or hypoxic (0.5% O2) conditions for 72 h while untreated or exposed to cediranib (2 uM), quinacrine (2 uM), or combined cediranib/quinacrine.
Neuro Oncol 2013 15, 1673-83. Cediranib (AZD2171) purchased from Selleck.
Inhibition of P-gp and Bcrp by cediranib. Accumulation of [3H]vin-blastine in MDR1-transfected cells and [3H]prazosin in Bcrp1-transfected cells in the presence of increasing concentrations of cediranib ranging from 0 to 40 μM is shown.
J Pharmacol Exp Ther 2012 341, 386-395 . Cediranib (AZD2171) purchased from Selleck.
Ba/F3 cell lines expressing the recombinant TEL/kinase domain fusion protein for FGFR1-4 .Cells were grown in RPMI 1640 containing 10% FBS and 500 ng/mL puromycin. The parental Ba/F3 cell line transduced with an empty vector was grown in 10 ng/mL IL-3 (R & D systems). Cell viability was assessed at 72 hours using the Cell Titer 96 Aqueous One Solution (Promega). Data were plotted as percent viability relative to vehicle-treated cells and are shown as mean (±SD) from 3 experiments.
Dr. Mikhail Menshikov of Cardiology Research Center. Cediranib (AZD2171) purchased from Selleck.
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|Description||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.|
Cediranib inhibits VEGF-stimulated proliferation with IC50 of 0.4 nM. Cediranib suppresses PDGF-AA with IC50 of 0.04 μM in MG63 cell lines. Cediranib has been shown to block Flt1-associated kinase with IC50 of 5 nM and VEGF-C and VEGF-D receptor Flt-4 with IC50 less than 3 nM. In addition, the IC50 values for inhibition of c-Kit and PDGFRβ tyrosine kinase are 2 nM and 5 nM respectively. Furthermore, no inhibition of enzyme activity is observed when 10 μM Cediranib is assayed with 100 μM ATP against AMPK, Chk1 Akt/PKB and others. Micromolar concentrations of Cediranib are needed to prevent tumor cell proliferation in vitro. 
|In vivo||Cediranib even suppresses tubule sprouting at subnanomolar concentrations and inhibits VEGF-induced angiogenesis. Cediranib causes hypertrophy in bone growth plate and prevents luteal development in ovary. These are physiological processes that are dependent upon angiogenesis. Cediranib shows broad spectrum activity in human tumor models at doses that are well tolerated.  Besides, Cediranib causes regression of vascular tissues in human lung tumor xenografts. |
Kinase inhibition:Cediranib is dissolved in DMSO at a concentration of 10 mM. All enzyme assays are run at, or just below, the respective Km for ATP (0.2 - 30 μM). The inhibitory activity of Cediranib is determined against a range of recombinant tyrosine kinases [KDR, Flt-1, Flt-4, c-Kit, PDGFRα, PDGFRβ, CSF-1R, Flt-3, FGFR1, Src, Abl, epidermal growth factor receptor (EGFR), ErbB2, Aurora A, and Aurora B] using ELISA. Selectivity versus CDK2 and CDK4 serine/threonine kinases is examined using scintillation proximity assays with a retinoblastoma substrate and [γ-sup>33P]ATP. Activity of Cediranib is compared to MAPK kinase (MEK), which shows dual specificity. It is determined using a MAPK substrate, [γ-33P]ATP, and paper capture/scintillation counting.
|In vitro||DMSO||90 mg/mL (199.77 mM)|
|In vivo||5% DMSO+50% PEG 300+5% Tween+ddH2O||5mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02498613||Recruiting||Estrogen Receptor Negative|HER2/Neu Negative|Metastatic Pancreatic Adenocarcinoma|Pancreatic Adenocarcinoma|Progesterone Receptor Negative|Recurrent Breast Carcinoma|Recurrent Non-Small Cell Lung Carcinoma|Recurrent Pancreatic Carcinoma|Recurrent Small Cell Lung Carcinoma|Stage III Pancreatic Cancer|Stage IIIA Breast Cancer|Stage IIIA Non-Small Cell Lung Cancer|Stage IIIA Small Cell Lung Carcinoma|Stage IIIB Non-Small Cell Lung Cancer|Stage IIIB Small Cell Lung Carcinoma|Stage IIIC Breast Cancer|Stage IV Breast Cancer|Stage IV Non-Small Cell Lung Cancer|Stage IV Small Cell Lung Carcinoma|Stage IVA Pancreatic Cancer|Stage IVB Pancreatic Cancer|Triple-Negative Breast Carcinoma||National Cancer Institute (NCI)|AstraZeneca||April 2016||Phase 2|
|NCT02681237||Not yet recruiting||Ovarian Cancer||University Health Network, Toronto|AstraZeneca||March 2016||--|
|NCT02502266||Recruiting||Fallopian Tube Clear Cell Adenocarcinoma|Fallopian Tube Endometrioid Adenocarcinoma|Fallopian Tube Mucinous Adenocarcinoma|Fallopian Tube Serous Adenocarcinoma|Fallopian Tube Transitional Cell Carcinoma|Ovarian Clear Cell Adenocarcinoma|Ovarian Endometrioid Adenocarcinoma|Ovarian Mucinous Adenocarcinoma|Ovarian Seromucinous Carcinoma|Ovarian Serous Adenocarcinoma|Ovarian Transitional Cell Carcinoma|Primary Peritoneal Serous Adenocarcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Undifferentiated Fallopian Tube Carcinoma|Undifferentiated Ovarian Carcinoma||National Cancer Institute (NCI)||February 2016||Phase 2|Phase 3|
|NCT02446600||Recruiting||Fallopian Tube Clear Cell Adenocarcinoma|Fallopian Tube Transitional Cell Carcinoma|Ovarian Clear Cell Adenocarcinoma|Ovarian Endometrioid Tumor|Ovarian Seromucinous Carcinoma|Ovarian Serous Tumor|Ovarian Transitional Cell Carcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Undifferentiated Fallopian Tube Carcinoma|Undifferentiated Ovarian Carcinoma||National Cancer Institute (NCI)|AstraZeneca||February 2016||Phase 3|
|NCT02345265||Recruiting||BRCA1 Gene Mutation|BRCA2 Gene Mutation|Fallopian Tube Endometrioid Adenocarcinoma|Fallopian Tube Serous Adenocarcinoma|High Grade Ovarian Serous Adenocarcinoma|Ovarian Endometrioid Tumor|Primary Peritoneal Serous Adenocarcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma||National Cancer Institute (NCI)||December 2015||Phase 2|
|NCT02340611||Recruiting||Ovarian Cancer||University Health Network, Toronto|AstraZeneca||June 2015||Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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