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Cediranib (AZD217)

VEGFR inhibitor receptor,highly potent CAS# 288383-20-0

Cediranib (AZD217)

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Chemical Properties of Cediranib (AZD217)

Cas No. 288383-20-0 SDF Download SDF
PubChem ID 9933475 Appearance Powder
Formula C25H27FN4O3 M.Wt 450.51
Type of Compound N/A Storage Desiccate at -20°C
Synonyms AZD2171
Solubility DMSO : ≥ 49 mg/mL (108.77 mM)
H2O : < 0.1 mg/mL (insoluble)
*"≥" means soluble, but saturation unknown.
Chemical Name 4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxy-7-(3-pyrrolidin-1-ylpropoxy)quinazoline
SMILES CC1=CC2=C(N1)C=CC(=C2F)OC3=NC=NC4=CC(=C(C=C43)OC)OCCCN5CCCC5
Standard InChIKey XXJWYDDUDKYVKI-UHFFFAOYSA-N
Standard InChI InChI=1S/C25H27FN4O3/c1-16-12-17-19(29-16)6-7-21(24(17)26)33-25-18-13-22(31-2)23(14-20(18)27-15-28-25)32-11-5-10-30-8-3-4-9-30/h6-7,12-15,29H,3-5,8-11H2,1-2H3
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Cediranib (AZD217)

DescriptionCediranib is a highly potent inhibitor of VEGFR with IC50 value of <1 nM.
TargetsVEGFR2/KDRc-KitVEGFR3/FLT4VEGFR1/FLT1PDGFRβFGFR1
IC500.5 nM2 nM≤3 nM5 nM5 nM26 nM

Protocol

Kinase Assay [1]
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 Assay [1]
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 Administration [1]
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.

Cediranib (AZD217) Dilution Calculator

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Preparing Stock Solutions of Cediranib (AZD217)

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.2197 mL 11.0985 mL 22.1971 mL 44.3941 mL 55.4927 mL
5 mM 0.4439 mL 2.2197 mL 4.4394 mL 8.8788 mL 11.0985 mL
10 mM 0.222 mL 1.1099 mL 2.2197 mL 4.4394 mL 5.5493 mL
50 mM 0.0444 mL 0.222 mL 0.4439 mL 0.8879 mL 1.1099 mL
100 mM 0.0222 mL 0.111 mL 0.222 mL 0.4439 mL 0.5549 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Cediranib (AZD217)

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.

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References on Cediranib (AZD217)

Efficacy of targeted therapy for metastatic renal cell carcinoma in the elderly patient population.[Pubmed:24819320]

Clin Genitourin Cancer. 2014 Oct;12(5):354-8.

INTRODUCTION/BACKGROUND: Targeted therapy has become the mainstay of treatment for mRCC. The efficacy of this therapy in the older population is poorly understood. PATIENTS AND METHODS: Data from patients with mRCC treated with first-line anti-VEGF therapy were collected through the International mRCC Database Consortium from 12 centers. Patient characteristics, data on second-line therapy, and outcomes including treatment duration and overall survival, were evaluated using summary statistics and multivariate analysis. RESULTS: All patients (n = 1381) were treated with front-line targeted therapy; 144 (10%) were 75 years old or older. Six patients (4%) were favorable risk, 99 patients (69%) intermediate risk, and 39 patients (27%) poor risk according to Heng Journal of Clinical Oncology 2009 prognostic factors. The initial treatment for those >/= 75 years of age was sunitinib (n = 98), sorafenib (n = 35), bevacizumab (n = 7), and AZD217 (n = 4). Twenty-three percent of older patients and 39% of the younger patients went on to receive second-line therapy (P < .0001). The overall response rate, median treatment duration, and overall survival for the older versus younger group were 18% versus 25% (P = .0975), 5.5 months versus 7.5 months (P = .1388), and 16.8 months versus 19.7 months (P = .3321), respectively. When adjusted for poor prognostic factors, age 75 years and older was not found to be associated with poorer overall survival (hazard ratio [HR], 1.002; 95% confidence interval [CI], 0.781-1.285) or shorter treatment duration (HR, 1.018; 95% CI, 0.827-1.252). The retrospective study design was the primary limitation. CONCLUSION: The use of advanced age as a selection criterion for targeted therapy requires further study, with data suggesting no clinically meaningful differences in overall response rate, treatment duration, and overall survival between older and younger age groups.

Description

Cediranib (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.

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