Cediranib
Cediranib
CAS: 288383-20-0
Molecular Formula: C25H27FN4O3
Cediranib - Names and Identifiers
| 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 |
Cediranib - Physico-chemical Properties
| 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. |
Cediranib - Introduction
Cediranib (AZD2171) is a highly effective VEGFR(KDR) inhibitor, IC50 is <1 nM, and also inhibits Flt1/4,IC50 is 5 nM/≤ 3 nM. In addition, it also has similar inhibitory activity on c-Kit and PDGFRβ, and its selectivity to VEGFR is 36 times, 110 times and 1000 times higher than PDGFR-α, CSF-1R and Flt3 respectively. Phase 3.
Last Update：2022-10-16 17:24:17
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