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1mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
Cediranib (also called NSC732208; AZD2171, tentative trade name Recenti), an indole ether quinazoline derivative, is a potent and oral VEGFR (vascular endothelial growth factor receptors) inhibitor with potential antitumor activity. In HUVEC cells, it exhibits >1000-fold selectivity for inhibiting VEGFR over PDGFR-α, CSF-1R, and Flt3. It also inhibits VEGFR with an IC50 of<1 nM. AstraZeneca is developing cediranib as an oral medication for the treatment of cancers, including colorectal, kidney, and non-small cell lung cancer.
Targets |
Flt-1 (IC50 = 5 nM); KDR (IC50 = 1 nM); Flt-4 (IC50 = 3 nM); PDGFRα (IC50 = 36 nM); PDGFRβ (IC50 = 5 nM); c-Kit (IC50 = 2 nM)
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ln Vitro |
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ln Vivo |
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Enzyme Assay |
In DMSO, cediranib is dissolved at a 10 mM concentration. Every enzyme test is conducted at or slightly below the corresponding Km for ATP (0.2 - 30 μM). Cediranib's inhibitory activity is assessed using ELISA against a variety of recombinant tyrosine kinases, including KDR, Flt-1, Flt-4, c-Kit, PDGFRα, PDGFRβ, CSF-1R, Flt-3, FGFR1, Src, Abl, and the epidermal growth factor receptor (EGFR), ErbB2, Aurora A, and Aurora B. In scintillation proximity assays, selectivity against CDK2 and CDK4 serine/threonine kinases is investigated using retinoblastoma substrate and [γ-sup>33P]ATP. Cediranib's activity is contrasted with that of MAPK kinase (MEK), demonstrating dual specificity. A MAPK substrate, [γ-33P]ATP, and paper capture/scintillation counting are used to determine it.
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Cell Assay |
After incubating for four days, 3H-thymidine incorporation is measured to assess the proliferation of the HUVEC cell line in the presence and absence of growth factors. PDGF-AA stimulates the PDGFRα homodimer's signaling specifically, leading to the proliferation of MG63 osteosarcoma cells. For a duration of 24 hours, HUVEC and MG63 osteosarcoma cells are cultured in DMEM without phenol red, which also contains 1% charcoal stripped FCS, 2 mM glutamine, and 1% nonessential amino acids. After adding cediranib or the vehicle along with 50 ng/mL of PDGF-AA ligand, the plates are incubated for an additional 72 hours. Bromodeoxyuridine ElISA is used to measure cellular proliferation.
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Animal Protocol |
Rats: Cediranib (1.25–5 mg/kg/day) or vehicle is given orally to six-week-old female Wistar-derived Alderley Park rats (n = 5) once a day for 28 days. To investigate the effects of compound withdrawal, five more rats per group are treated for 28 days with either a vehicle or Cediranib (5 mg per kg per day) and then kept untreated for an additional 28 days. H&E is used to stain sections of the femorotibial joints and ovaries in histologic paraffin wax. Growth plate areas from the femur and tibia in each joint are combined for a morphometric image analysis of the femorotibial sections, which allows for an analysis of the impact of compound treatment. Morphometric analysis is also used to determine the area of corpora lutea in ovary sections stained with H&E.
Mice: Mice with human lung tumor xenografts Calu-6 (0.2±0.01 cm3) are chosen on day 0 and given a chronic dose of Cediranib (6 mg/kg daily, p.o.) or a vehicle. Six to fifteen tumors per group are collected on days 1, 2, 7, 14, and 21 four hours following the last Cediranib or vehicle dose. The next step is to use a chromagen end point or fluorescence immunostaining to detect CD31 in sections. |
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References |
Molecular Formula |
C25H27FN4O3
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Molecular Weight |
450.51
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Exact Mass |
450.21
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Elemental Analysis |
C, 66.65; H, 6.04; F, 4.22; N, 12.44; O, 10.65.
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CAS # |
288383-20-0
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Related CAS # |
Cediranib maleate;857036-77-2
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Appearance |
white solid powder
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SMILES |
CC1=CC2=C(N1)C=CC(=C2F)OC3=NC=NC4=CC(=C(C=C43)OC)OCCCN5CCCC5
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InChi Key |
XXJWYDDUDKYVKI-UHFFFAOYSA-N
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InChi Code |
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
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Chemical Name |
4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxy-7-(3-pyrrolidin-1-ylpropoxy)quinazoline
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Synonyms |
AZD2171; NSC 732208; NSC732208; AZD 2171; NSC-732208; AZD-2171; Brand name: Recentin
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (4.44 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2 mg/mL (4.44 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 5% DMSO+50% PEG 300+5% Tween+ddH2O: 5 mg/kg |
Preparing Stock Solutions | 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 | 0.2220 mL | 1.1099 mL | 2.2197 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT00750841 | Active Recruiting |
Drug: cediranib | Solid Tumors | AstraZeneca | September 9, 2008 | Phase 1 |
NCT01391962 | Active Recruiting |
Drug: Cediranib Drug: Sunitinib |
Sarcoma, Alveolar Soft Part | National Cancer Institute (NCI) |
July 18, 2011 | Phase 2 |
NCT03570437 | Active Recruiting |
Drug: Paclitaxel Drug: Cediranib |
Endometrial Neoplasms Carcinosarcoma |
University of Manchester | May 17, 2018 | Phase 2 |
NCT02974621 | Active Recruiting |
Drug: Cediranib Drug: Cediranib Maleate |
Recurrent Glioblastoma | National Cancer Institute (NCI) |
December 7, 2017 | Phase 2 |
NCT01364051 | Active Recruiting |
Drug: Cediranib Drug: Cediranib Maleate |
Refractory Malignant Solid Neoplasm Metastatic Melanoma |
National Cancer Institute (NCI) |
May 25, 2011 | Phase 1 |
AZD2171 inhibits VEGF-stimulated KDR phosphorylation in human endothelial cells.Cancer Res.2005 May 15;65(10):4389-400. td> |
AZD2171 inhibits tubule growthin vitro. HUVECs and human fibroblasts were obtained as commercial cocultures (AngioKit, TCS Cellworks).Cancer Res.2005 May 15;65(10):4389-400. td> |
AZD2171 inhibits VEGF-induced angiogenesisin vivo.Cancer Res.2005 May 15;65(10):4389-400. td> |
Consequences of inhibiting VEGF signaling and physiologic angiogenesisin vivo: effect of AZD2171 on bone morphogenesis and ovarian cycling in young female rats.Cancer Res.2005 May 15;65(10):4389-400. td> |
AZD2171 inhibits human tumor xenograft growth at doses that are well tolerated.Cancer Res.2005 May 15;65(10):4389-400. td> |
AZD2171 causes vascular regression in Calu-6 lung tumor xenografts.Cancer Res.2005 May 15;65(10):4389-400. td> |