Cediranib (NSC-732208; AZD-2171)

Alias: AZD2171; NSC 732208; NSC732208; AZD 2171; NSC-732208; AZD-2171; Brand name: Recentin
Cat No.:V0517 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.
Cediranib (NSC-732208; AZD-2171) Chemical Structure CAS No.: 288383-20-0
Product category: VEGFR
This product is for research use only, not for human use. We do not sell to patients.
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Other Forms of Cediranib (NSC-732208; AZD-2171):

  • Cediranib maleate
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

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.

Biological Activity I Assay Protocols (From Reference)
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)
ln Vitro

Cediranib has an IC50 of 0.4 nM, which inhibits proliferation stimulated by VEGF. With an IC50 of 0.04 μM, cediranib inhibits PDGF-AA in MG63 cell lines. With an IC50 of less than 3 nM, cediranib has been demonstrated to block VEGF-C and VEGF-D receptor Flt-4 as well as Flt1-associated kinase. Furthermore, 2 nM and 5 nM, respectively, are the IC50 values for the inhibition of c-Kit and PDGFRβ tyrosine kinase. Additionally, when 100 μM ATP and 10 μM Cediranib are tested against AMPK, Chk1 Akt/PKB, and other enzymes, no inhibition of enzyme activity is seen. Cediranib must be used at micromolar concentrations in vitro to stop the growth of tumor cells.[1]

ln Vivo
Cediranib even prevents VEGF-induced angiogenesis and suppresses tubule sprouting at subnanomolar concentrations. Cediranib stops the development of the luteal phase in the ovary and causes hypertrophy in the bone growth plate. Angiogenesis is a prerequisite for these physiological processes. In well-tolerated dosages, cediranib exhibits broad spectrum activity in human tumor models.[1] Furthermore, in human lung tumor xenografts, cediranib induces vascular tissue regression.[2]
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.
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.
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.
References

[1]. Cancer Res . 2005 May 15;65(10):4389-400.

[2]. Pediatr Blood Cancer . 2012 Apr;58(4):566-71.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C25H27FN4O3
Molecular Weight
450.51
Exact Mass
450.21
Elemental Analysis
C, 66.65; H, 6.04; F, 4.22; N, 12.44; O, 10.65.
CAS #
288383-20-0
Appearance
white solid powder
SMILES
CC1=CC2=C(N1)C=CC(=C2F)OC3=NC=NC4=CC(=C(C=C43)OC)OCCCN5CCCC5
InChi Key
XXJWYDDUDKYVKI-UHFFFAOYSA-N
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
Chemical Name
4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxy-7-(3-pyrrolidin-1-ylpropoxy)quinazoline
Synonyms
AZD2171; NSC 732208; NSC732208; AZD 2171; NSC-732208; AZD-2171; Brand name: Recentin
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
DMSO: ~90 mg/mL (~199.8 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In Vivo)
5% DMSO+50% PEG 300+5% Tween+ddH2O: 5 mg/kg
 (Please use freshly prepared in vivo formulations for optimal results.)
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.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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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.
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Clinical Trial Information
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
Biological Data
  • Cediranib (AZD2171)

    AZD2171 inhibits VEGF-stimulated KDR phosphorylation in human endothelial cells.2005 May 15;65(10):4389-400.

  • Cediranib (AZD2171)

    AZD2171 inhibits tubule growthin vitro. HUVECs and human fibroblasts were obtained as commercial cocultures (AngioKit, TCS Cellworks).2005 May 15;65(10):4389-400.

  • Cediranib (AZD2171)

    AZD2171 inhibits VEGF-induced angiogenesisin vivo.2005 May 15;65(10):4389-400.

  • Cediranib (AZD2171)

    Consequences of inhibiting VEGF signaling and physiologic angiogenesisin vivo: effect of AZD2171 on bone morphogenesis and ovarian cycling in young female rats.2005 May 15;65(10):4389-400.

  • Cediranib (AZD2171)

    AZD2171 inhibits human tumor xenograft growth at doses that are well tolerated.2005 May 15;65(10):4389-400.

  • Cediranib (AZD2171)

    AZD2171 causes vascular regression in Calu-6 lung tumor xenografts.2005 May 15;65(10):4389-400.

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