Art. -Nr.: HY-10205

Cediranib

(Synonyms: AZD2171)

13 Cited Publications

Kundenbewertung

Based on 13 publication(s) in Google Scholar

Cediranib (AZD2171) is a highly potent, orally available and blood-brain barrier permeability VEGFR tyrosine kinase inhibitor with IC₅₀s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.

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Reinheit: 99.87%
CAS. Nr.: 288383-20-0
Formel: C₂₅H₂₇FN₄O₃
Molecular Weight:450.51

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Cediranib Chemical Structure

CAS. Nr.: 288383-20-0

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (13)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

Flt-1

5 nM (IC₅₀)

KDR

1 nM (IC₅₀)

Flt-4

3 nM (IC₅₀)

PDGFRα

36 nM (IC₅₀)

PDGFRβ

5 nM (IC₅₀)

c-Kit

2 nM (IC₅₀)

Alle VEGFR Isoform-spezifische Produkte anzeigen :

Alle PDGFR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	1.71 nM Compound: Cediranib	Antiproliferative activity against VEGFR2-transformed mouse BaF3 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay Antiproliferative activity against VEGFR2-transformed mouse BaF3 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay	[PMID: 37429211]
HCT-116	IC₅₀	1.91 μM Compound: Cediranib	Antitumor activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay Antitumor activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay	[PMID: 37429211]
HeLa	IC₅₀	7.67 μM Compound: Cediranib	Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay	[PMID: 29624387]
HT-29	IC₅₀	3.45 μM Compound: Cediranib	Antitumor activity against human HT-29 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay Antitumor activity against human HT-29 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay	[PMID: 37429211]
HUVEC	ED₅₀	0.012 μM Compound: 5, ZD-2171	Inhibition of VEGF-stimulated HUVEC cell proliferation treated before 2 hrs of VEGF challenge assessed after 3 days by [3H]thymidine incorporation assay Inhibition of VEGF-stimulated HUVEC cell proliferation treated before 2 hrs of VEGF challenge assessed after 3 days by [3H]thymidine incorporation assay	[PMID: 19101155]
HUVEC	IC₅₀	1.2 nM Compound: Cediranib	Antiproliferative activity against HUVEC assessed as inhibition of human recombinant VEGF165-induced proliferation preincubated for 2 hrs followed by VEGF165 addition measured after 48 hrs by cell counting analysis Antiproliferative activity against HUVEC assessed as inhibition of human recombinant VEGF165-induced proliferation preincubated for 2 hrs followed by VEGF165 addition measured after 48 hrs by cell counting analysis	10.1039/C5MD00191A
HUVEC	IC₅₀	2.14 nM Compound: Cediranib	Antiproliferative activity against VEGF-stimulated HUVEC assessed as inhibition of cell proliferation incubated for 3 days by MTT assay Antiproliferative activity against VEGF-stimulated HUVEC assessed as inhibition of cell proliferation incubated for 3 days by MTT assay	[PMID: 37429211]
MDA-MB-231	IC₅₀	3.82 μM Compound: Cediranib	Antitumor activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay Antitumor activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay	[PMID: 37429211]
MDA-MB-468	IC₅₀	3.91 μM Compound: Cediranib	Antitumor activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay Antitumor activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay	[PMID: 37429211]
OVCAR-3	IC₅₀	5.87 μM Compound: Cediranib	Antitumor activity against human OVCAR-3 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay Antitumor activity against human OVCAR-3 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay	[PMID: 37429211]
SK-OV-3	IC₅₀	6.68 μM Compound: Cediranib	Antitumor activity against human SK-OV-3 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay Antitumor activity against human SK-OV-3 cells assessed as inhibition of cell proliferation incubated for 3 days by MTT assay	[PMID: 37429211]

In Vitro

In human umbilical vein endothelial cells, Cediranib inhibits VEGF-stimulated proliferation and KDR phosphorylation with IC₅₀ values of 0.4 and 0.5 nM, respectively. In a fibroblast/endothelial cell coculture model of vessel sprouting, Cediranib also reduces vessel area, length, and branching at subnanomolar concentrations^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Once-daily oral administration of Cediranib ablates experimental (VEGF-induced) angiogenesis and inhibits endochondral ossification in bone or corpora luteal development in ovary; physiologic processes that are highly dependent upon neovascularization. The growth of established human tumor xenografts (colon, lung, prostate, breast, and ovary) in athymic mice is inhibited dose-dependently by Cediranib, with chronic administration of 1.5 mg per kg per day producing statistically significant inhibition in all models. A histologic analysis of Calu-6 lung tumors treated with Cediranib reveals a reduction in microvessel density within 52 hours that becomes progressively greater with the duration of treatment. These changes are indicative of vascular regression within tumors^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 288383-20-0
Appearance Solid
Molecular Weight 450.51
Formel C₂₅H₂₇FN₄O₃
Color White to yellow
SMILES

FC1=C(OC2=C(C(C=C3OCCCN4CCCC4)=NC=N2)C=C3OC)C=CC5=C1C=C(C)N5
Synonyms

AZD2171
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (13)

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Journal Impact Factor

Nat Nanotechnol

Nanoparticles reach metastatic tumours via enhanced permeability of adjacent vessels. [Abstract]

2026 Jun;21(6):880-891. PMID: 42286217
Cell Stem Cell

Generation of Human PSC-Derived Kidney Organoids with Patterned Nephron Segments and a De Novo Vascular Network. [Abstract]

2019 Sep 5;25(3):373-387.e9. PMID: 31303547
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Leukemia

A Perturb-seq map of a differentiation hub reveals synergistic vulnerabilities in KMT2A-rearranged acute myeloid leukemia. [Abstract]

2026 Mar 25. PMID: 41882099
Neuro Oncol

Loss of endothelial programmed cell death 10 activates glioblastoma cells and promotes tumor growth. [Abstract]

2016 Apr;18(4):538-48. PMID: 26254477
Biomaterials

Hacking macrophage-associated immunosuppression for regulating glioblastoma angiogenesis. [Abstract]

2018 Apr;161:164-178. PMID: 29421553
J Med Chem

Discovery and Mechanistic Study of Novel Mycobacterium tuberculosis ClpP1P2 Inhibitors. [Abstract]

2023 Dec 28;66(24):16597-16614. PMID: 38088921
Antioxidants (Basel)

A Novel SIRT1 Activator Hydroxygenkwanin Alleviates Osteoporosis by Inhibiting Ferroptosis and Lactylation in Skeletal Stem/Progenitor Cells. [Abstract]

2026 May 12;15(5):612. PMID: 42193234
Sci Signal

Pleiotrophin promotes vascular abnormalization in gliomas and correlates with poor survival in patients with astrocytomas. [Abstract]

2015 Dec 8;8(406):ra125. PMID: 26645582
Life Sci

The antihypertensive effect of Alizarin is achieved by activating VEGFR2/eNOS pathway, attenuating oxidative stress-induced mitochondrial damage and premature senescence. [Abstract]

2024 Jun 23:122862. PMID: 38917872
Eur J Pharmacol

Cediranib ameliorates portal hypertensive syndrome via inhibition of VEGFR-2 signaling in cirrhotic rats. [Abstract]

2024 Feb 5:964:176278. PMID: 38158116
Discov Oncol

Aberrant expression of MRAS and HEG1 as the biomarkers for osimertinib resistance in LUAD. [Abstract]

2024 Nov 19;15(1):678. PMID: 39560891
Biomed Res Int

Cediranib Induces Apoptosis, G1 Phase Cell Cycle Arrest, and Autophagy in Non-Small-Cell Lung Cancer Cell A549 In Vitro. [Abstract]

2021 Mar 29:2021:5582648. PMID: 33860036

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 20 mg/mL (44.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2 mg/mL (4.44 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2 mg/mL (4.44 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Kinase Assay^[1]

The inhibitory activity of Cediranib is determined against a range of recombinant tyrosine kinases [KDR, Flt-1, Flt-4, c-Kit, PDGFR-α, PDGFR-β, CSF-1R, Flt-3, FGFR1, Src, Abl, epidermal growth factor receptor (EGFR), ErbB2, Aur-A, and Aur-B] using ELISA methodology^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[1]

Proliferation of MG63 osteosarcoma cells is induced by PDGF-AA, which selectively activates PDGFR-α homodimer signaling. 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 reincubated for 72 hours. Cellular proliferation is determined using a bromodeoxyuridine^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

Rats: Young female Alderley Park rats (6 weeks of age, Wistar derived, n=5) are dosed orally, once daily for 28 days with Cediranib (1.25-5 mg per kg per day) or vehicle. Additional rats (five per group) are treated with Cediranib (5 mg per kg per day) or vehicle for 28 days and maintained for a further 28 days without treatment, to examine the effect of compound withdrawal. Histologic paraffin wax sections of the femorotibial joints and ovaries are stained with H&E. Morphometric image analysis of femorotibial sections is done, with growth plate areas from both the femur and tibia in each joint being combined for an analysis of the effect of compound treatment. The area of corpora lutea in H&E-stained ovary sections is similarly determined by morphometric analysis^[1].

Mice: Mice bearing established Calu-6 human lung tumor xenografts (0.2±0.01 cm³) are selected (day 0) and treated chronically with Cediranib (6 mg per kg per day, p.o.) or vehicle. Tumors are collected (6-15 per group) 4 hours after the last dose of Cediranib or vehicle, on days 1, 2, 7, 14, and 21. CD31 is then detected in sections using a chromagen end point or fluorescent immunostaining^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Wedge SR, et al. AZD2171: a highly potent, orally bioavailable, vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for the treatment of cancer. Cancer Res, 2005, 65(10), 4389-4400. [Content Brief]

[2]. Zhang L, et al. Pleiotrophin promotes vascular abnormalization in gliomas and correlates with poor survival in patients with astrocytomas. Sci Signal. 2015 Dec 8;8(406):ra125. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2197 mL	11.0985 mL	22.1971 mL	55.4927 mL
	5 mM	0.4439 mL	2.2197 mL	4.4394 mL	11.0985 mL
	10 mM	0.2220 mL	1.1099 mL	2.2197 mL	5.5493 mL
	15 mM	0.1480 mL	0.7399 mL	1.4798 mL	3.6995 mL
	20 mM	0.1110 mL	0.5549 mL	1.1099 mL	2.7746 mL
	25 mM	0.0888 mL	0.4439 mL	0.8879 mL	2.2197 mL
	30 mM	0.0740 mL	0.3700 mL	0.7399 mL	1.8498 mL
	40 mM	0.0555 mL	0.2775 mL	0.5549 mL	1.3873 mL

Keywords

Cediranib

13 Cited Publications

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Cediranib

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Publications Citing Use of MedChemExpress (MCE) Cediranib

Alle VEGFR Isoform-spezifische Produkte anzeigen

Alle PDGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (13)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Cediranib Related Classifications

HY-10205 Related Classifications