ZD-4190 是血管内皮细胞生长因子受体 2 (VEGFR2) 和表皮生长因子受体 (EGFR) 信号传导的抑制剂,用于治疗癌症。
产品描述
ZD-4190 is a inhibitor of the vascular endothelial cell growth factor receptor 2 (VEGFR2) and of epidermal growth factor receptor (EGFR) signalling, used for the treatment of cancer.
体外活性
ZD4190 can prevent outgrowth of malignant cells when the tumour burden is below a critical threshold.
体内活性
ZD4190 (100 mg/kg, p.o.) effectively delays MDA-MB-435 tumor growth in mice. In ZD4190-treated tumors, 18F-FPPRGD2 uptake has decreased significantly relative to baseline by 26.74 8.12% (p<0.05) on day 1 and by 41.19 6.63% (p<0.01) on day 3, then has returned to baseline on day 7. Tumor uptake of 18F-FLT has also decreased on both day 1 and day 3 after initiation of ZD4190 treatment. However, ZD4190 does not significantly change 18F-FDG uptake in tumors, compared with the control group.
动物实验
ZD4190 was administered by gavage suspended in 1% polysorbate 80 at 50 mg/kg 24 h after tumour cell implantation for a maximum of 22 days. Control rodents were gavaged with the vehicle only and a third group was untreated. In preliminary experiments, rodents were killed on alternate days so that the effect of ZD4190 on tumour outgrowth could be assessed and subsequently the treatment response was evaluated at day 9 or 22. At least five rodents were included in each treatment group.
Cas No.
413599-62-9
分子式
C19H16BrFN6O2
分子量
459.279
储存和溶解度
DMSO:20.83 mg/mL (45.35 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years