857036-77-2
Cediranib Maleate
CAS: 857036-77-2
Molecular Formula: C25H27FN4O3·C4H4O4
857036-77-2 - Names and Identifiers
857036-77-2 - Physico-chemical Properties
| Molecular Formula | C25H27FN4O3·C4H4O4 |
| Molar Mass | 566.59 |
| Melting Point | 198.3-200.08 °C (polymorph) |
| Storage Condition | Room Temprature |
| Physical and Chemical Properties | Bioactive Cediranib maleate (AZD-2171 maleate) is a highly selective, orally active VEGFR2 inhibitor with IC50 values for Flt1,KDR,Flt4,PDGFRα,PDGFRβ,c-Kit less than 1, less than 3,5,5,36,2nM, respectively. |
| In vitro study | In human umbilical vein endothelial cells, Cediranib inhibits VEGF-stimulated proliferation and KDR phosphorylation with IC 50 values of 0.4 and 0.5 nM, respectively. In a fibroblast/endothelial cell coculture model of vessel sprouting, Cediranib also reduces vessel area, length, and branching at subnanomolar concentrations. |
| In vivo study | Once-daily oral administration of Cediranib ablates experimental (VEGF-induced) angiogenesis and inhibits endochondral ossification in bone or corpora luteal development in ovary; physiologic processes that are highly dependent upon neovascularization. The growth of established human tumor xenografts (colon, lung, prostate, breast, and ovary) in athymic mice is inhibited dose-dependently by Cediranib, with chronic administration of 1.5 mg per kg per day producing statistically significant inhibition in all models. A histologic analysis of Calu-6 lung tumors treated with Cediranib reveals a reduction in microvessel density within 52 hours that becomes progressively greater with the duration of treatment. These changes are indicative of vascular regression within tumors. |
857036-77-2 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.765 ml | 8.825 ml | 17.65 ml |
| 5 mM | 0.353 ml | 1.765 ml | 3.53 ml |
| 10 mM | 0.176 ml | 0.882 ml | 1.765 ml |
| 5 mM | 0.035 ml | 0.176 ml | 0.353 ml |
Last Update：2024-01-02 23:10:35
857036-77-2 - Uses and synthesis methods
in vitro studies
In human umbilical vein endothelial cells, Cediranib inhibits VEGF-stimulated proliferation and KDR phosphorylation with IC 50 values of 0.4 and 0.5 nM, respectively. In a fibroblast/endothelial cell coculture model of vessel sprouting, Cediranib also reduces vessel area, length, and branching at subnanomolar concentrations.
In vivo studies
Once-daily oral administration of Cediranib ablates experimental (VEGF-induced) angiogenesis and inhibits endochondral ossification in bone or corpora luteal development in ovary; physiologic processes that are highly dependent upon neovascularization. The growth of established human tumor xenografts (colon, lung, prostate, breast, and ovary) in athymic mice is inhibited dose-dependently by Cediranib, with chronic administration of 1.5 mg per kg per day producing statistically significant inhibition in all models. A histologic analysis of Calu-6 lung tumors treated with Cediranib reveals a reduction in microvessel density within 52 hours that becomes progressively greater with the duration of treatment. These changes are indicative of vascular regression within tumors.
Last Update：2024-04-09 21:01:54
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