Name | Cediranib |
Synonyms | AZD2171 Recentin Cediranib Cadiranib Cediranib R Cediranib(AZD2171) Cadiranib (AZD2171) 4-(4-Fluoro-2-methylindol-5-yloxy)-6-methoxy-7-[3-(pyrrolidin-1-yl)propoxy]quinazoline 4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxy-7-(3-pyrrolidin-1-ylpropoxy)quinazoline |
CAS | 288383-20-0 |
EINECS | 670-946-2 |
InChI | InChI=1/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 |
Molecular Formula | C25H27FN4O3 |
Molar Mass | 450.51 |
Density | 1.285 |
Melting Point | 135-138°C |
Boling Point | 626.6±55.0 °C(Predicted) |
Flash Point | 332.73°C |
Solubility | DMSO 90 mg/mL Water <1 mg/mL Ethanol <1 mg/mL |
Vapor Presure | 0mmHg at 25°C |
Appearance | Solid |
Color | White to Off-White |
pKa | 16.14±0.30(Predicted) |
Storage Condition | Sealed in dry,Store in freezer, under -20°C |
Refractive Index | 1.642 |
In vitro study | Cediranib inhibited bFGF and EGF with an IC50 of 0.5 and 0.11 μm, respectively. In the MG63 cell line, Cediranib inhibited by PDGF-AA with an IC50 of 0.04 μm. Cediranib inhibited Flt-1 of the associated kinase with an IC50 of 5 nM, and Cediranib inhibited VEGF-C and VEGF-D of the receptor with an IC50 of less than 3 nM. In addition, cediranib inhibited c-Kit and PDGFR-β tyrosine kinase with IC50 of 2 and 5 nM, respectively. In vitro, micromolar concentrations of cediranib can directly inhibit tumor cell proliferation. Subnanomolar concentrations of Cediranib blocked tubule production and inhibited VEGF-induced angiogenesis in vivo. |
In vivo study | Cediranib causes skeletal overgrowth, prevents the production of corpus luteum in the ovary, and inhibits angiogenesis-dependent physiological processes. Cediranib was very effective in human xenograft models in a dose-dependent manner. In addition, cediranib causes vascular regression in human lung cancer xenografts. |