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413599-62-9

中文名称 413599-62-9
英文名称 ZD-4190
CAS 413599-62-9
分子式 C19H16BrFN6O2
分子量 459.27
MOL 文件 413599-62-9.mol
更新日期 2024/08/06 14:59:37
413599-62-9 结构式 413599-62-9 结构式

基本信息

中文别名
化合物ZD-4190
英文别名
ZD-4190
ZD-4190
ZD 4190
ZD4190
4-Quinazolinamine, N-(4-bromo-2-fluorophenyl)-6-methoxy-7-[2-(1H-1,2,3-triazol-1-yl)ethoxy]-

物理化学性质

储存条件-20°C储存
溶解度DMSO : 20.83 mg/mL (45.35 mM);Water : < 0.1 mg/mL (insoluble)
形态Solid
颜色White to off-white

常见问题列表

生物活性
ZD-4190是VEGF RTK抑制剂,对KDR和Flt-1的IC50值分别为29 ± 4 nM和708 ± 63 nM。
靶点
TargetValue
KDR
()
Flt-1
()
体外研究

ZD4190 exhibits cytotoxic activity against the tumor cells.

体内研究

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. ZD4190 (50 mg/kg, p.o.) prevents outgrowth of residual tumour in a muscle model of minimal residual carcinoma. ZD4190 (12.5-100 mg/kg, p.o.) produces a dose-dependent reduction in K(trans) in PC-3 prostate tumors. At 100 mg/kg, ZD4190 reduces K(trans) in PC-3 tumors by 31% following 2 doses and by 53% following 8 doses.

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