Cediranib (AZD2171)

Catalog No.S1017 Synonyms: NSC-732208

Cediranib (AZD2171) Chemical Structure

Molecular Weight(MW): 450.51

Cediranib (AZD2171) is a highly potent VEGFR(KDR) inhibitor with IC50 of <1 nM, also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM, similar activity against c-Kit and PDGFRβ, 36-, 110-fold and >1000-fold selective more for VEGFR than PDGFR-α, CSF-1R and Flt3 in HUVEC cells. Phase 3.

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Cited by 27 Publications

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Biological Activity

Description Cediranib (AZD2171) is a highly potent VEGFR(KDR) inhibitor with IC50 of <1 nM, also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM, similar activity against c-Kit and PDGFRβ, 36-, 110-fold and >1000-fold selective more for VEGFR than PDGFR-α, CSF-1R and Flt3 in HUVEC cells. Phase 3.
Targets
VEGFR2/KDR [1]
(HUVECs)
c-Kit [1]
(HUVECs)
VEGFR3/FLT4 [1]
(HUVECs)
VEGFR1/FLT1 [1]
(HUVECs)
PDGFRβ [1]
(HUVECs)
0.5 nM 2 nM <=3 nM 5 nM 5 nM
In vitro

Cediranib inhibits VEGF-stimulated proliferation with IC50 of 0.4 nM. Cediranib suppresses PDGF-AA with IC50 of 0.04 μM in MG63 cell lines. Cediranib has been shown to block Flt1-associated kinase with IC50 of 5 nM and VEGF-C and VEGF-D receptor Flt-4 with IC50 less than 3 nM. In addition, the IC50 values for inhibition of c-Kit and PDGFRβ tyrosine kinase are 2 nM and 5 nM respectively. Furthermore, no inhibition of enzyme activity is observed when 10 μM Cediranib is assayed with 100 μM ATP against AMPK, Chk1 Akt/PKB and others. Micromolar concentrations of Cediranib are needed to prevent tumor cell proliferation in vitro. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HUVEC cell MXrQdo9tcW[ncnH0bY9vKGG|c3H5 Mk\rN{Bl[Xm| NHXUZ5dKdmirYnn0bY9vKG:oIG\FS2Yue3SrbYXsZZRm\CCKVW\FR{Bk\WyuIIDyc4xq\mW{YYTpc44hfHKnYYTl[EBj\W[xcnWgNkBpenNib3[gWmVITiClaHHscIVv\2ViYYPz[ZN{\WRiYX\0[ZIhOyCmYYnzJIJ6KFt|SG30bJlucWSrbnWgbY5kd3Kyb4LheIlwdiCjc4PhfUwhTUR3ME2xNkBvVQ>? Mom2NVkyODFzNUW=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
BRCA2 / BRCA1 / RAD51 ; 

PubMed: 31092693     


Western blot of HDR factors in ovarian (IGROV1, SKOV3, and PEO14) and breast (MCF7 and MDA231) cancer cell lines treated with increasing doses of cediranib in culture (n = 3 independent experiments).

p-VEGFR1 / p-VEGFR3 / p-AKT / p-ERK ; 

PubMed: 19755510     


Hep-1 hepatocellular carcinoma cells pretreated with or without cediranib (100 nmol/L), were left untreated (SF; lanes 1, 6), or were stimulated with 10% FBS (lanes 2, 7), 10 ng VEGF-A (lanes 3, 8), 50 ng VEGF-B (lanes 4, 9), or 50 ng VEGF-C (lanes 5, 10) for 10 min. Immunoblotting was done on 50 µg of total cell lysate per well and probed with the appropriate phospho-specific (p) antibody. Experiments were done in triplicate.

31092693 19755510
In vivo Cediranib even suppresses tubule sprouting at subnanomolar concentrations and inhibits VEGF-induced angiogenesis. Cediranib causes hypertrophy in bone growth plate and prevents luteal development in ovary. These are physiological processes that are dependent upon angiogenesis. Cediranib shows broad spectrum activity in human tumor models at doses that are well tolerated. [1] Besides, Cediranib causes regression of vascular tissues in human lung tumor xenografts. [2]

Protocol

Kinase Assay:[1]
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Kinase inhibition:

Cediranib is dissolved in DMSO at a concentration of 10 mM. All enzyme assays are run at, or just below, the respective Km for ATP (0.2 - 30 μM). The inhibitory activity of Cediranib is determined against a range of recombinant tyrosine kinases [KDR, Flt-1, Flt-4, c-Kit, PDGFRα, PDGFRβ, CSF-1R, Flt-3, FGFR1, Src, Abl, epidermal growth factor receptor (EGFR), ErbB2, Aurora A, and Aurora B] using ELISA. Selectivity versus CDK2 and CDK4 serine/threonine kinases is examined using scintillation proximity assays with a retinoblastoma substrate and [γ-sup>33P]ATP. Activity of Cediranib is compared to MAPK kinase (MEK), which shows dual specificity. It is determined using a MAPK substrate, [γ-33P]ATP, and paper capture/scintillation counting.
Cell Research:[1]
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  • Cell lines: HUVEC cell line
  • Concentrations: 10 μM
  • Incubation Time: 72 hours
  • Method: The proliferation of the HUVEC cell line is evaluated in the presence and absence of growth factors by measuring 3H-thymidine incorporation following a 4-day incubation period. Proliferation of MG63 osteosarcoma cells is induced by PDGF-AA, which selectively activates signaling of the PDGFRα homodimer. HUVEC and MG63 osteosarcoma 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 incubated for another 72 hours. Cellular proliferation is determined using bromodeoxyuridine ELISA.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: PC-3, Calu-6, SKOV-3, MDA-MB-231, and SW620 tumors in female nude (nu/nu genotype) mice
  • Formulation: Suspended in 1% (w/v) aqueous polysorbate 80
  • Dosages: 0.75-6 mg/kg/day
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 90 mg/mL (199.77 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+50% PEG 300+5% Tween+ddH2O
For best results, use promptly after mixing.
5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 450.51
Formula

C25H27FN4O3

CAS No. 288383-20-0
Storage powder
in solvent
Synonyms NSC-732208

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02484404 Recruiting Drug: Olaparib|Drug: Cediranib|Drug: MEDI4736 Colorectal Neoplasms|Breast Neoplasms National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) June 29 2015 Phase 1|Phase 2
NCT01391962 Recruiting Drug: Cediranib|Drug: Sunitinib Sarcoma Alveolar Soft Part National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) July 19 2011 Phase 2
NCT01337401 Active not recruiting Drug: Cediranib|Drug: Placebo Alveolar Soft-part Sarcoma Institute of Cancer Research United Kingdom|Royal Marsden NHS Foundation Trust July 2011 Phase 2
NCT01160926 Terminated Drug: AZD6244|Drug: Cediranib (AZD2171) Rectal Cancer The Christie NHS Foundation Trust|Cancer Research UK|AstraZeneca July 2010 Phase 1
NCT00503412 Completed Drug: AZD2171 Advanced Solid Metastatic Tumor AstraZeneca November 2005 Phase 1
NCT00502060 Completed Drug: AZD2171|Drug: ZD1839 Advanced Tumor AstraZeneca August 2004 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID