Cediranib maleate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种高效、口服生物可利用的泛 VEGFR 抑制剂，对 VEGFR1、2、3 的 IC50 分别为 1、5、3 nM。

A highly potent, orally bioavailable, pan-VEGFR inibitor with IC50 of 1, 5, 3 nM for VEGFR1, 2, 3, respectively; also inhibits c-Kit and PDGFRβ with IC50 of 2 and 5 nM, >36-fold selectivity over PDGFR-α, >1000-fold over Flt-3 and EGFR; inhibits VEGF-stimulated proliferation and KDR phosphorylation with IC50 of 0.4 and 0.5 nM in human umbilical vein endothelial cells; inhibits angiogenesis, neovascular survival and tumor growth in vivo. Ovarian Cancer Phase 3 Clinical.

In human umbilical vein endothelial cells, Cediranib inhibits VEGF-stimulated proliferation and KDR phosphorylation with IC50 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.

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.

AZD-2171 maleate | AZD 2171 maleate

Angiogenesis

VEGFR

VEGFR

Cancer

Ovarian Cancer

857036-77-2

566.5775

C29H31FN4O7

>98% (HPLC)

DMSO: ≥ 45 mg/mL

CC1=CC2=C(N1)C=CC(=C2F)OC3=NC=NC4=CC(=C(C=C43)OC)OCCCN5CCCC5.C(=CC(=O)O)C(=O)O

Quinazoline, 4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxy-7-[3-(1-pyrrolidinyl)propoxy]-, (2Z)-2-butenedioate (1:1)

(-20℃)

With Ice Pack

≥ 2 years