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.
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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||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+50% PEG 300+5% Tween+ddH2O
For best results, use promptly after mixing.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02484404||Recruiting||Drug: Olaparib|Drug: Cediranib|Drug: MEDI4736||Colorectal Neoplasms|Breast Neoplasms||National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)||June 29 2015||Phase 1|Phase 2|
|NCT01391962||Recruiting||Drug: Cediranib|Drug: Sunitinib||Sarcoma Alveolar Soft Part||National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)||July 19 2011||Phase 2|
|NCT01337401||Active not recruiting||Drug: Cediranib|Drug: Placebo||Alveolar Soft-part Sarcoma||Institute of Cancer Research United Kingdom|Royal Marsden NHS Foundation Trust||July 2011||Phase 2|
|NCT01160926||Terminated||Drug: AZD6244|Drug: Cediranib (AZD2171)||Rectal Cancer||The Christie NHS Foundation Trust|Cancer Research UK|AstraZeneca||July 2010||Phase 1|
|NCT00503412||Completed||Drug: AZD2171||Advanced Solid Metastatic Tumor||AstraZeneca||November 2005||Phase 1|
|NCT00502060||Completed||Drug: AZD2171|Drug: ZD1839||Advanced Tumor||AstraZeneca||August 2004||Phase 1|
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