Cediranib (AZD2171)

ArtNr	S1017-5000
Hersteller	Selleckchem
CAS-Nr.	288383-20-0
Menge	5 g
Quantity options	10 mg 100 mg 1 g 10 g 10 mM/1 mL 200 mg 25 mg 5 mg 50 mg 5 g
Kategorie	Oncology Neuroscience Neural Signaling Neural Development Inhibitors & Compound Libraries Small Molecules By Organ Lung Cancer Bladder Cancer Head & Neck Cancer Heart & Blood Cancer Bone Cancer Uterine, Ovarian & Cervical Cancer
Typ	Inhibitors
Specific against	other
Smiles	CC1=CC2=C(N1)C=CC(=C2F)OC3=NC=NC4=CC(=C(C=C43)OC)OCCCN5CCCC5
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	NSC-732208
Similar products	Cediranib
Lieferbar
Manufacturer - Targets	FLT1
Storage Conditions	2 years -80 in solvent
Molecular Weight	450, 51
Administration	Orally
Animal Models	PC-3, Calu-6, SKOV-3, MDA-MB-231, and SW620 tumors in female nude (nu/nu genotype) mice
Cell lines	HUVEC cell line
Clinical Trials	Cediranib is currently being evaluated in a phase II clinical trial for the treatment of advanced solid tumors.
Concentrations	10 uM
Dosages	0.75-6 mg/kg/day
Formulation	Suspended in 1% (w/v) aqueous polysorbate 80
IC50	0.5 nM, 0.5 nM, 0.5 nM, 0.5 nM, 0.5 nM, 0.5 nM
In vitro	Cediranib inhibits VEGF-stimulated proliferation with IC50 of 0.4 nM. Cediranib suppresses PDGF-AA with IC50 of 0.04 uM 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 PDGFRbeta tyrosine kinase are 2 nM and 5 nM respectively. Furthermore, no inhibition of enzyme activity is observed when 10 uM Cediranib is assayed with 100 uM 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]
Incubation Time	72 hours
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 uM). The inhibitory activity of Cediranib is determined against a range of recombinant tyrosine kinases [KDR, Flt-1, Flt-4, c-Kit, PDGFRalpha, PDGFRbeta, 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 [gamma-sup>33P]ATP. Activity of Cediranib is compared to MAPK kinase (MEK), which shows dual specificity. It is determined using a MAPK substrate, [gamma-33P]ATP, and paper capture/scintillation counting.
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 PDGFRalpha 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.
Solubility (25C)	DMSO 90 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL
Information	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, 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. Cediranib (AZD2171) induces autophagic vacuole accumulation. Phase 3.
Chemical Name	4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazoline

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