| Name | Cediranib maleate |
| Description | Cediranib maleate (AZD2171 maleate) is an orally active and highly potent VEGF family receptor tyrosine kinase (VEGFR2) inhibitor that inhibits Flt1, KDR, Flt4, PDGFRα, PDGFRβ, and c-Kit, and up-regulates MHC-I through transcriptional modulation in the study of ovarian cancer. |
| In vitro | Cediranib maleate (AZD2171) is a highly selective, orally active VEGFR2 inhibitor with IC50 values of 5 nM, ＜1 nM, ＜3 nM, 36 nM, 5 nM, and 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, and c-Kit, respectively. in human umbilical vein endothelial cells. Cediranib maleate was able to block VEGF-stimulated proliferation and KDR phosphorylation with IC50 values of 0.4 nM and 0.5 nM, respectively.In a fibroblast/endothelial cell co-culture model of vascular sprouting, Cediranib maleate reduced vascular area, length, and branching at subnanomolar concentrations. [1] |
| In vivo | Once-daily oral administration of Cediranib maleate abrogated experimental (VEGF-induced) angiogenesis and inhibited endochondral ossification in bone or luteinization in the ovary; these processes are highly dependent on neointima formation. The growth of human tumor xenografts (colon, lung, prostate, mammary gland, and ovary) established in thymus-free mice was dose-dependently inhibited by Cediranib maleate, and long-term administration at a dose of 1.5 mg/kg/day produced statistically significant inhibition in all models. Histological analysis of Calu-6 lung tumors treated with Cediranib maleate showed a decrease in microvessel density over 52 hours and a further decrease with treatment duration. These changes indicate that the vascularity within the tumor is regressing. [1] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 40 mg/mL (70.6 mM), Sonication is recommended.
H2O : 1 mg/mL (1.76 mM), Sonication is recommended.
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| Keywords | AZD-2171 | AZD2171 | AZD 2171 |
| Inhibitors Related | Stavudine | Aceglutamide | Hemin | Tamoxifen | Cysteamine hydrochloride | Guanidine hydrochloride | Hydroxychloroquine | Enzalutamide | Paeonol | Naringin | Alginic acid | Sildenafil citrate |
United States
