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Cediranib

Catalog No. T2500 CAS 288383-20-0

Synonyms: AZD2171, NSC-732208

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

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Cediranib, CAS 288383-20-0

Pack Size	Availability	Price/USD
2 mg	In stock	$ 35.00
5 mg	In stock	$ 57.00
10 mg	In stock	$ 84.00
25 mg	In stock	$ 138.00
50 mg	In stock	$ 187.00
100 mg	In stock	$ 267.00
200 mg	In stock	$ 487.00
500 mg	In stock	$ 782.00
1 mL * 10 mM (in DMSO)	In stock	$ 63.00

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Purity: 99.94%

Purity: 99.78%

Purity: 97.21%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Cediranib (AZD2171) (AZD2171) is a highly potent (IC50 < 1 nmol/L) ATP-competitive inhibitor of recombinant KDR tyrosine kinase in vitro, also inhibits Flt1/4 (IC50: 5 nM/≤3 nM), similar activity against PDGFRβ and c-Kit, selective more for VEGFR than PDGFR-α (36-fold), CSF-1R (110-fold), and Flt3 (1000-fold) in HUVEC cells.
Targets&IC50	FLK1:5 nM, FLT4:≤3 nM
In vitro	Cediranib exhibits highly effective and dose-dependent activity in human xenograft models. Additionally, Cediranib induces vascular regression in human lung cancer xenografts. It causes excessive skeletal growth, obstructs the production of corpora lutea in the ovaries, and inhibits physiological processes that are dependent on angiogenesis.
In vivo	In vitro, Cediranib directly inhibits the proliferation of tumor cells and blocks microtubule formation, while also suppressing angiogenesis induced by VEGF in vivo. Cediranib exhibits inhibition against bFGF (IC50: 0.5 μM) and EGF (IC50: 0.11 μM), and in the MG63 cell line, it inhibits PDGF-AA (IC50: 0.04 μM). Furthermore, Cediranib suppresses Flt-1 associated kinases (IC50: 5 nM) and exhibits inhibitory effects on the VEGF-C and VEGF-D receptors, Flt-4 (IC50 < 3 nM), in addition to inhibiting the tyrosine kinases c-Kit (IC50: 2 nM) and PDGFR-β (IC50: 5 nM).
Kinase Assay	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	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)

Synonyms	AZD2171, NSC-732208
Molecular Weight	450.51
Formula	C25H27FN4O3
CAS No.	288383-20-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 83 mg/mL (184.2 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

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.

Citations

1. Zhang J, Guo H, Wang L, et al.Cediranib enhances the transcription of MHC-I by upregulating IRF-1.Biochemical Pharmacology.2024: 116036.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library Anti-Cancer Clinical Compound Library FDA-Approved Kinase Inhibitor Library Highly Selective Inhibitor Library Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Drug Repurposing Compound Library Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library

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Keywords

Cediranib 288383-20-0 Angiogenesis Autophagy Tyrosine Kinase/Adaptors VEGFR FLT PDGFR c-Kit Platelet-derived growth factor receptor Vascular endothelial growth factor receptor inhibit AZD2171 NSC-732208 NSC732208 AZD 2171 NSC 732208 AZD-2171 Inhibitor inhibitor

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