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Cediranib

Catalog No. T2500 CAS 288383-20-0

Synonyms: AZD 2171, Platelet-derived growth factor receptor, AZD2171, Vascular endothelial growth factor receptor, PDGFR, AZD-2171, Cediranib, inhibit, VEGFR, NSC-732208, Autophagy, Inhibitor

Cediranib (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

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Purity: 98%

Biological Description

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Storage & Solubility Information

Description	Cediranib (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	Flt4:≤3 nM, Flt1:5 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	AZD 2171, Platelet-derived growth factor receptor, AZD2171, Vascular endothelial growth factor receptor, PDGFR, AZD-2171, Cediranib, inhibit, VEGFR, NSC-732208, Autophagy, Inhibitor
Molecular Weight	450.514
Formula	C25H27FN4O3
CAS No.	288383-20-0

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

H2O: <1 mg/mL

DMSO: 83 mg/mL (184.2 mM)

Ethanol: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library Autophagy Compound Library Cytokine Inhibitor Library Anti-Obesity Compound Library Anti-Pancreatic Cancer Compound Library Inhibitor Library Drug-induced Liver Injury (DILI) Compound Library Fluorochemical Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library

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