ZD-4190 is a potent, orally available inhibitor of the vascular endothelial cell growth factor receptor 2 (VEGFR2) and of epidermal growth factor receptor (EGFR) signalling, used for the treatment ofcancer.

ZD4190 exhibits cytotoxic activity against the tumor cells^[2].

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^[1]. ZD4190 (50 mg/kg, p.o.) prevents outgrowth of residual tumour in a muscle model of minimal residual carcinoma^[2]. 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^[3].

459.27

Solid

C₁₉H₁₆BrFN₆O₂

413599-62-9

Room temperature in continental US; may vary elsewhere.

DMSO : 20.83 mg/mL(45.35 mM;Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.08 mg/mL (4.53 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (4.53 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。