Cediranib

Cediranib, also known as AZD-2171, is a potent and selective VEGF inhibitor with antineoplastic activities. Competing with adenosine triphosphate, cediranib binds to and inhibits all three vascular endothelial growth factor receptor (VEGF-1, -2, -3) tyrosine kinases, thereby blocking VEGF-signaling, angiogenesis, and tumor cell growth.

Product information

CAS Number: 288383-20-0

Molecular Weight: 450.51

Formula: C25H27FN4O3

Synonym:

AZD2171

AZD 2171

AZD-2171

AZD2171 free base

Cediranib

Related CAS Number:

857036-77-2 (Cediranib maleate)

Chemical Name: 4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazoline

Smiles: CC1=CC2=C(F)C(=CC=C2N1)OC1=NC=NC2=CC(OCCCN3CCCC3)=C(C=C21)OC

InChiKey: XXJWYDDUDKYVKI-UHFFFAOYSA-N

InChi: InChI=1S/C25H27FN4O3/c1-16-12-17-19(29-16)6-7-21(24(17)26)33-25-18-13-22(31-2)23(14-20(18)27-15-28-25)32-11-5-10-30-8-3-4-9-30/h6-7,12-15,29H,3-5,8-11H2,1-2H3

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: 90 mg/mL(199.77 mM). Water: Insoluble.

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Cediranib inhibits VEGF-stimulated proliferation with IC50 of 0.4 nM. Cediranib suppresses PDGF-AA with IC50 of 0.04 μM 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 PDGFRβ tyrosine kinase are 2 nM and 5 nM respectively. Furthermore, no inhibition of enzyme activity is observed when 10 μM Cediranib is assayed with 100 μM ATP against AMPK, Chk1 Akt/PKB and others. Micromolar concentrations of Cediranib are needed to prevent tumor cell proliferation in vitro.

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. Besides, Cediranib causes regression of vascular tissues in human lung tumor xenografts.

References:

1. Morton CL, et al. Pediatr Blood Cancer, 2012, 58(4), 566-571.
2. Wedge SR, et al. Cancer Res, 2005, 65(10), 4389-4400.

Products are for research use only. Not for human use.