Cediranib (AZD217) (Synonyms: AZD 2171, ZD 2171) |
| Catalog No.GC16421 |
Cediranib (AZD217) (AZD2171) is a highly potent, orally available VEGFR tyrosine kinase inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 288383-20-0
Sample solution is provided at 25 µL, 10mM.
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Cediranib (also known as AZD2171) is a highly potent KDR tyrosine kinase inhibitor that ATP-competitively inhibits recombinant KDR tyrosine kinase as well as other members of vascular endothelial growth factor receptor (VEGFR) family, including Flt-1 (VEGFR-1) and Flt-4 (VEGFR-3) with the half maximal inhibition concentration IC50 values of <0.001 μmol/L, 0.005 μmol/L and <0.003 μmol/L respectively [1].
Cediranib also potently inhibits a few members of platelet-derived growth factor receptor (PDGFR) family, including c-Kit, PDGFR-β, PDGFR-α, CSF-1R and Flt-3, with IC50 values of 0.002 μmol/L, 0.005 μmol/L, 0.036 μmol/L, 0.11 μmol/L anf > 1 μmol/L respectively due to their similar structure to VEGFR family members [1].
References:
[1] Wedge SR, Kendrew J, Hennequin LF, Valentine PJ, Barry ST, Brave SR, Smith NR, James NH, Dukes M, Curwen JO, Chester R, Jackson JA, Boffey SJ, Kilburn LL, Barnett S, Richmond GH, Wadsworth PF, Walker M, Bigley AL, Taylor ST, Cooper L, Beck S, Jürgensmeier JM, Ogilvie DJ. AZD2171: a highly potent, orally bioavailable, vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for the treatment of cancer. Cancer Res. 2005 May 15;65(10):4389-400.
Kinase experiment: | The inhibitory activity of Cediranib is determined against a range of recombinant tyrosine kinases [KDR, Flt-1, Flt-4, c-Kit, PDGFR-α, PDGFR-β, CSF-1R, Flt-3, FGFR1, Src, Abl, epidermal growth factor receptor (EGFR), ErbB2, Aur-A, and Aur-B] using ELISA methodology[1]. |
Cell experiment: | Proliferation of MG63 osteosarcoma cells is induced by PDGF-AA, which selectively activates PDGFR-α homodimer signaling. Cells are cultured in DMEM without phenol red containing 1% charcoal stripped FCS, 2 mM glutamine, and 1% nonessential amino acids for 24 hours. Cediranib or vehicle is added with PDGF-AA ligand (50 ng/mL) and plates reincubated for 72 hours. Cellular proliferation is determined using a bromodeoxyuridine[1]. |
Animal experiment: | Rats: Young female Alderley Park rats (6 weeks of age, Wistar derived, n=5) are dosed orally, once daily for 28 days with Cediranib (1.25-5 mg per kg per day) or vehicle. Additional rats (five per group) are treated with Cediranib (5 mg per kg per day) or vehicle for 28 days and maintained for a further 28 days without treatment, to examine the effect of compound withdrawal. Histologic paraffin wax sections of the femorotibial joints and ovaries are stained with H&E. Morphometric image analysis of femorotibial sections is done, with growth plate areas from both the femur and tibia in each joint being combined for an analysis of the effect of compound treatment. The area of corpora lutea in H&E-stained ovary sections is similarly determined by morphometric analysis[1]. Mice: Mice bearing established Calu-6 human lung tumor xenografts (0.2±0.01 cm3) are selected (day 0) and treated chronically with Cediranib (6 mg per kg per day, p.o.) or vehicle. Tumors are collected (6-15 per group) 4 hours after the last dose of Cediranib or vehicle, on days 1, 2, 7, 14, and 21. CD31 is then detected in sections using a chromagen end point or fluorescent immunostaining[1]. |
References: [1]. Wedge SR, et al. AZD2171: a highly potent, orally bioavailable, vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for the treatment of cancer. Cancer Res, 2005, 65(10), 4389-4400. | |
| Cas No. | 288383-20-0 | SDF | |
| Synonyms | AZD 2171, ZD 2171 | ||
| Chemical Name | 4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxy-7-(3-pyrrolidin-1-ylpropoxy)quinazoline | ||
| Canonical SMILES | CC1=CC2=C(N1)C=CC(=C2F)OC3=NC=NC4=CC(=C(C=C43)OC)OCCCN5CCCC5 | ||
| Formula | C25H27FN4O3 | M.Wt | 450.51 |
| Solubility | ≥ 22.5mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2197 mL | 11.0985 mL | 22.1971 mL |
| 5 mM | 0.4439 mL | 2.2197 mL | 4.4394 mL |
| 10 mM | 0.222 mL | 1.1099 mL | 2.2197 mL |
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Quality Control & SDS
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- Purity: >99.50%
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Average Rating: 5 (Based on Reviews and 11 reference(s) in Google Scholar.)
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