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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 (Sigma-Aldrich) containing 1% charcoal stripped FCS, 2 mmol/L glutamine, and 1% nonessential amino acids (Invitrogen, Paisley, United Kingdom) for 24 hours. AZD2171 or vehicle was added with PDGF-AA ligand (50 ng/mL; Sigma-Aldrich) and plates reincubated for 72 hours. Cellular proliferation was determined using a bromodeoxyuridine ELISA (Roche Diagnostics Ltd., Lewes, United Kingdom). |
| 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 |
[5] Sahade et al. Future Oncol. Cediranib: a VEGF receptor tyrosine kinase inhibitor.
| Related VEGFR/PDGFR Products |
|---|
| Conbercept
Conbercept (KH902) is a monoclonal antibody targeting VEGFRA fused to the IGHG1 Fc fragment. Conbercept is produced by the fusion of the second C-LIKE of FLT1 and the third and fourth C-LIKE of KDR with IGHG1 Fc. |
| SU5208
SU5208 inhibits vascular endothelial growth factor receptor-2 (VEGFR2). |
| VEGFR-IN-1
VEGFR-IN-1 is a potent angiogenesis inhibitor with IC50s of 0.02, 0.18, 0.24 7.3, and 7 µM for KDR, Flt-1, c-Kit, EGF-R, and c-Src, respectively. |
| (Z)-Orantinib
(Z)-Orantinib ((Z)-SU6668) is a potent, selective, orally active and ATP competitive inhibitor of Flk‐1/KDR, PDGFRβ, and FGFR1, with IC50s of 2.1, 0.008, and 1.2 µM, respectively. |
| (Rac)-SAR131675
(Rac)-SAR131675 is the racemate of SAR131675. |
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