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Cediranib (AZD2171) VEGFR inhibitor

Name: Cediranib (AZD2171)
SKU: S1017
Availability: InStock
Rating: 5 (67 reviews)

Cat.No.S1017

Cediranib (AZD2171, NSC-732208) is a highly potent VEGFR(KDR) inhibitor with IC50 of <1 nM, also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM, and shows similar activity against c-Kit and PDGFRβ. It is 36-, 110-fold and >1000-fold more selective for VEGFR than PDGFR-α, CSF-1R and Flt3 in HUVEC cells. This compound induces autophagic vacuole accumulation and is in Phase 3.

Chemical Structure

Molecular Weight: 450.51

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.64%

99.64

Related Targets	EGFR PDGFR FGFR c-Met Src FLT3 HER2 c-Kit Bcr-Abl MEK BTK IGF-1R ALK Trk receptor Syk Axl CSF-1R c-RET FAK Mertk Tie-2 DYRK Tyro3 Ephrin receptor ROS1 Pyk2 RON DDR ACK Fer kinase
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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
HUVEC cell	Proliferation assay	3 days	Inhibition of VEGF-stimulated HUVEC cell proliferation treated before 2 hrs of VEGF challenge assessed after 3 days by [3H]thymidine incorporation assay, ED50=12 nM	19101155
HeLa	Function assay	4.5 hrs	Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay, IC50=7.67μM	29624387
DAOY	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
SJ-GBM2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
BT-37	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
NB-EBc1	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
Saos-2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
SK-N-SH	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
LAN-5	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
BT-12	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
Rh18	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
OHS-50	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
RD	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
MG 63 (6-TG R)	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
fibroblast cells	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	29435139
Rh30	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	29435139
Rh41	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	450.51	Formula	C₂₅H₂₇FN₄O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	288383-20-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	NSC-732208			Smiles	CC1=CC2=C(N1)C=CC(=C2F)OC3=NC=NC4=CC(=C(C=C43)OC)OCCCN5CCCC5

Solubility

In vitro
Batch:

DMSO : 90 mg/mL (199.77 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 50%PEG300 2 5%Tween80 3 40%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (11.10mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 500 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 400 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	VEGFR2/KDR ^[1] (HUVECs) 0.5 nM c-Kit ^[1] (HUVECs) 2 nM VEGFR3/FLT4 ^[1] (HUVECs) <=3 nM VEGFR1/FLT1 ^[1] (HUVECs) 5 nM PDGFRβ ^[1] (HUVECs) 5 nM FGFR1 ^[1] (HUVECs) 26 nM PDGFRα ^[1] (HUVECs) 36 nM
In vitro	Cediranib (AZD2171) inhibits VEGF-stimulated proliferation with IC50 of 0.4 nM and suppresses PDGF-AA with IC50 of 0.04 μM in MG63 cell lines. It 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 of this compound is assayed with 100 μM ATP against AMPK, Chk1 Akt/PKB and others. Micromolar concentrations are needed to prevent tumor cell proliferation in vitro. ^[1]
Kinase Assay	Kinase inhibition
Kinase Assay	Cediranib (AZD2171) is dissolved in DMSO at a concentration of 10 mM. All enzyme assays are run at, or just below, the respective K_m for ATP (0.2 - 30 μM). The inhibitory activity of this compound 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 it 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.
In vivo	Cediranib (AZD2171) even suppresses tubule sprouting at subnanomolar concentrations and inhibits VEGF-induced angiogenesis. This compound causes hypertrophy in bone growth plate and prevents luteal development in ovary. These are physiological processes that are dependent upon angiogenesis. It shows broad spectrum activity in human tumor models at doses that are well tolerated. ^[1] Besides, it causes regression of vascular tissues in human lung tumor xenografts. ^[2]
References	[1] https://pubmed.ncbi.nlm.nih.gov/15899831/ [2] https://pubmed.ncbi.nlm.nih.gov/21538824/

Applications

Methods	Biomarkers	Images	PMID
Western blot	BRCA2 / BRCA1 / RAD51 p-VEGFR1 / p-VEGFR3 / p-AKT / p-ERK		31092693

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04184518	Withdrawn	Uveal Melanoma\|Metastatic Cancer	Grupo Español Multidisciplinar de Melanoma\|MFAR	May 2020	Phase 2
NCT02484404	Recruiting	Colorectal Neoplasms\|Breast Neoplasms	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	June 29 2015	Phase 1\|Phase 2
NCT01391962	Active not recruiting	Sarcoma Alveolar Soft Part	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	July 18 2011	Phase 2
NCT01337401	Unknown status	Alveolar Soft-part Sarcoma	Institute of Cancer Research United Kingdom\|Royal Marsden NHS Foundation Trust	July 2011	Phase 2
NCT01160926	Terminated	Rectal Cancer	The Christie NHS Foundation Trust\|Cancer Research UK\|AstraZeneca	July 2010	Phase 1

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