Cediranib Inhibitor CAS No. 288383-20-0

Cat. No.	Name	Size	Price
KI0203	Cediranib	5 mg	$120
	Cediranib	10 mg	$193.6
	Cediranib	25 mg	$299.2
	Cediranib	50 mg	$475.2

Chemical Characteristic

Product Name	Cediranib
Synonyms	Recentin, AZD2171
CAS No.	288383-20-0
Molecular Weight	450.505
Formula	C₂₅H₂₇FN₄O₃
Chemical Name	4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazoline
Smiles	n1cnc(c2cc(c(cc12)OCCCN1CCCC1)OC)Oc1c(c2cc([nH]c2cc1)C)F
Chemical Structure

Biological activities

Cediranib is a potent inhibitor of vascular endothelial growth factor (VEGF) receptor tyrosine kinases. Cediranib inhibits VEGF-stimulated proliferation and VEGF receptor-2 phosphorylation with IC50 of 0.4 and 0.5 nM, respectively.^[1] Cediranib inhibits VEGF-A-stimulated VEGFR-1 activation in AG1-G1-Flt1 cells with an IC50 of 1.2 nM. Cediranib also demonstrates significant activity against wild-type c-K_{it in cellular phosphorylation assays and in a stem cell factor-induced proliferation assay with IC50 of ∼2 and 13 nM, respectively. Cediranib inhibits PDGFR-β and -α receptor phosphorylation with IC50 ranging from 12 to 32 nM tumor cell lines including vascular smooth muscle cells (VSMC) and a fibroblast line. Cediranib prevents PDGF-BB-stimulated cellular proliferation in human VSMC (vascular smooth muscle cells) and osteosarcoma cells with IC50 of 32 and 64 nM, respectively. ^[2] Cediranib inhibits ATPase activity of ABCB1 (P-glycoprotein) in a dose-dependent manner.^[3] When given during tumor growth, cediranib reduces the diameters of the draining lymphatic vessels, the number of tumor cells arriving in the draining lymph node, and the incidence of lymphatic metastasis. ^[4] Cediranib dose-dependently inhibits VEGFR-2 phosphorylation and its downstream signaling in human umbilical vascular endothelial cells. The IC50 of cediranib is 500 nM against the proliferation of human umbilical vascular endothelial cells. ^[5] Once-daily oral administration of cediranib ablates experimental (VEGF-induced) angiogenesis in vivo and inhibits endochondral ossification in bone or corpora luteal development in ovary. Cediranib with a chronic administration of 1.5 mg/kg /day dose-dependently inhibits the growth of established human tumor xenografts (colon, lung, prostate, breast, and ovary) in athymic mice.^[1] Oral administration of cediranib (??.5 mg/kg/day) markedly reduces phosphorylation of wild-type c-K_{it in NCI-H526 tumor xenografts tumor-bearing nude mice. Cediranib at a dose of 6 mg/kg prevents ligand-induced PDGFR-β (platelet-derived growth factor receptors) phosphorylation in murine lung tissue by 55%. In contrast, in C6 rat glial tumor xenografts in mice, ligand induced phosphorylation of both PDGFR-α and -β is blocked by 46-61% by cediranib at 0.75 mg/kg. ^[2]}}

References

[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. [2] Brave SR,et al. Assessing the activity of cediranib, a VEGFR-2/3 tyrosine kinase inhibitor, against VEGFR-1 and members of the structurally related PDGFR family. Mol Cancer Ther. 2011, 10(5): 861-873. [3] Tao LY, et al. Cediranib (recentin, AZD2171) reverses ABCB1- and ABCC1-mediated multidrug resistance by inhibition of their transport function. Cancer Chemother Pharmacol. 2009, 64(5): 961-969. [4] Padera TP,et al. Differential response of primary tumor versus lymphatic metastasis to VEGFR-2 and VEGFR-3 kinase inhibitors cediranib and vandetanib. Mol Cancer Ther. 2008, 7(8): 2272-2279. [5] Gomez-Rivera F, et al. The tyrosine kinase inhibitor, AZD2171, inhibits vascular endothelial growth factor receptor signaling and growth of anaplastic thyroid cancer in an orthotopic nude mouse model. Clin Cancer Res. 2007, 13(15 Pt 1): 4519-4527.

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