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Cediranib (AZD2171) inhibited VEGFR2 and KDR phosphorylation with IC50s of 0.4 and 0.5 nM, respectively. Cediranib significantly increased survival of mice wth glioblastoma by decreasing tumor vessel permeability, normalizing perivascular cell coverage, and thinning of the basement membrane, thus controlling edema. Cediranib demonstrated potent antitumor and antiangiogenic efficacy in the murine renal cell carcinoma model.
| Cell Experiment | |
|---|---|
| Cell lines | HUVEC cells line |
| Preparation method | Inhibition of growth factor–mediated cellular proliferation. HUVEC proliferation in the presence and absence of growth factors was evaluated following a 4-day incubation by 3H-thymidine incorporation, as described previously. Proliferation of MG63 osteosarcoma cells was induced by PDGF-AA, which selectively activates PDGFR-α homodimer signaling. Cells were cultured in DMEM without phenol red containing 1% charcoal stripped FCS, 2 mmol/L glutamine, and 1% nonessential amino acids for 24 hours. AZD2171 or vehicle was added with PDGF-AA ligand (50 ng/mL) and plates reincubated for 72 hours. Cellular proliferation was determined using a bromodeoxyuridine ELISA. |
| Concentrations | 0~10 μ M |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | female Alderley Park mice or rat bearing human tumor xenografts model |
| Formulation | suspended in 1% (w/v) aqueous polysorbate 80 (polyoxyethylene; sorbitan mono-oleate in deionized water)(mice) / 0.5% (w/v) hydroxypropyl methylcellulose solution containing 0.1% (w/v) aqueous polysorbate 80(rat) |
| Dosages | 0.75-6 mg/kg |
| Administration | orally |
| Molecular Weight | 450.51 |
| Formula | C25H27FN4O3 |
| CAS Number | 288383-20-0 |
| Solubility (25°C) | DMSO ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[2] Sahade et al. Future Oncol. Cediranib: a VEGF receptor tyrosine kinase inhibitor.
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| Axitinib
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| Nintedanib
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