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Cediranib is a highly potent and ATP-competitive inhibitor of VEGFR2 (IC50 = <1 nM). Cediranib also potently inhibits PDGFR1, VEGFR3, VEGFR1, c-Kit, PDGFR2 and FGFR1 (IC50 values are 2, 3, 5, 5, 26 and 36 nM, respectively), and inhibits CSF-1R, Src, and Abl (IC50 values are 110, 130 and 260 nM, respectively). Cediranib induces hypoxia, prevents VEGF-induced angiogenesis and suppresses homology-directed DNA repair (HDR) factors BRCA1/2 and RAD51. Cediranib decreases cell motility, proliferation and cell viability. Cediranib is active in vivo.
Cediranib is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 450.51. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.22 mL||11.1 mL||22.2 mL|
|5 mM||0.44 mL||2.22 mL||4.44 mL|
|10 mM||0.22 mL||1.11 mL||2.22 mL|
|50 mM||0.04 mL||0.22 mL||0.44 mL|
References are publications that support the biological activity of the product.
Wedge et al (2005) AZD2171: a highly potent, orally bioavailable, vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for the treatment of cancer. Cancer Res. 65 4389 PMID: 15899831
Kaplan et al (2019) Cediranib suppresses homology-directed DNA repair through down-regulation of BRCA1/2 and RAD51. Sci.Transl.Med. 11 PMID: 31092693
Momeny et al (2020) Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells Eur.J.Pharmacol. 882 PMID: 32593665
If you know of a relevant reference for Cediranib, please let us know.
Keywords: Cediranib, Cediranib supplier, tyrosine, kinases, inhibitors, inhibits, potent, VEGFR, PDGFR, FGFR, kinase, insert, domain, vascular, endothelial, growth, factor, platelet, derived, fibroblast, receptor, hypoxia, angiogenesis, BRCA1, proliferation, motility, 7454, Tocris Bioscience
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