Cediranib (AZD2171)

Catalog No.S1017

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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Cediranib (AZD2171) Chemical Structure

Cediranib (AZD2171) Chemical Structure
Molecular Weight: 450.51

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  • Research Area
  • Inhibition Profile

Product Description

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)

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IC50 0.5 nM 2 nM <=3 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]
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]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

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 Assay: [1]

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.

Animal Study: [1]

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

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Wedge SR, et al. Cancer Res, 2005, 65(10), 4389-4400.

[2] Morton CL, et al. Pediatr Blood Cancer, 2012, 58(4), 566-571.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02498613 Recruiting Estrogen Receptor Negative|HER2/Neu Negative|Metastatic Pancreatic Adenocarcinoma|Pancreatic Adenocarcinoma|Progesterone Receptor Negative|Recurren  ...more Estrogen Receptor Negative|HER2/Neu Negative|Metastatic Pancreatic Adenocarcinoma|Pancreatic Adenocarcinoma|Progesterone Receptor Negative|Recurrent Breast Carcinoma|Recurrent Non-Small Cell Lung Carcinoma|Recurrent Pancreatic Carcinoma|Recurrent Small Cell Lung Carcinoma|Stage III Pancreatic Cancer|Stage IIIA Breast Cancer|Stage IIIA Non-Small Cell Lung Cancer|Stage IIIA Small Cell Lung Carcinoma|Stage IIIB Non-Small Cell Lung Cancer|Stage IIIB Small Cell Lung Carcinoma|Stage IIIC Breast Cancer|Stage IV Breast Cancer|Stage IV Non-Small Cell Lung Cancer|Stage IV Small Cell Lung Carcinoma|Stage IVA Pancreatic Cancer|Stage IVB Pancreatic Cancer|Triple-Negative Breast Carcinoma National Cancer Institute (NCI)|AstraZeneca April 2016 Phase 2
NCT02681237 Not yet recruiting Ovarian Cancer University Health Network, Toronto|AstraZeneca March 2016 --
NCT02502266 Recruiting Fallopian Tube Clear Cell Adenocarcinoma|Fallopian Tube Endometrioid Adenocarcinoma|Fallopian Tube Mucinous Adenocarcinoma|Fallopian Tube Serous Ad  ...more Fallopian Tube Clear Cell Adenocarcinoma|Fallopian Tube Endometrioid Adenocarcinoma|Fallopian Tube Mucinous Adenocarcinoma|Fallopian Tube Serous Adenocarcinoma|Fallopian Tube Transitional Cell Carcinoma|Ovarian Clear Cell Adenocarcinoma|Ovarian Endometrioid Adenocarcinoma|Ovarian Mucinous Adenocarcinoma|Ovarian Seromucinous Carcinoma|Ovarian Serous Adenocarcinoma|Ovarian Transitional Cell Carcinoma|Primary Peritoneal Serous Adenocarcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Undifferentiated Fallopian Tube Carcinoma|Undifferentiated Ovarian Carcinoma National Cancer Institute (NCI) February 2016 Phase 2|Phase 3
NCT02446600 Recruiting Fallopian Tube Clear Cell Adenocarcinoma|Fallopian Tube Transitional Cell Carcinoma|Ovarian Clear Cell Adenocarcinoma|Ovarian Endometrioid Tumor|Ov  ...more Fallopian Tube Clear Cell Adenocarcinoma|Fallopian Tube Transitional Cell Carcinoma|Ovarian Clear Cell Adenocarcinoma|Ovarian Endometrioid Tumor|Ovarian Seromucinous Carcinoma|Ovarian Serous Tumor|Ovarian Transitional Cell Carcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Undifferentiated Fallopian Tube Carcinoma|Undifferentiated Ovarian Carcinoma National Cancer Institute (NCI)|AstraZeneca February 2016 Phase 3
NCT02345265 Recruiting BRCA1 Gene Mutation|BRCA2 Gene Mutation|Fallopian Tube Endometrioid Adenocarcinoma|Fallopian Tube Serous Adenocarcinoma|High Grade Ovarian Serous A  ...more BRCA1 Gene Mutation|BRCA2 Gene Mutation|Fallopian Tube Endometrioid Adenocarcinoma|Fallopian Tube Serous Adenocarcinoma|High Grade Ovarian Serous Adenocarcinoma|Ovarian Endometrioid Tumor|Primary Peritoneal Serous Adenocarcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma National Cancer Institute (NCI) December 2015 Phase 2

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Chemical Information

Download Cediranib (AZD2171) SDF
Molecular Weight (MW) 450.51
Formula

C25H27FN4O3

CAS No. 288383-20-0
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms NSC-732208
Solubility (25°C) * In vitro DMSO 90 mg/mL (199.77 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 5% DMSO+50% PEG 300+5% Tween+ddH2O 5mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name 4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazoline

Tech Support

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