ZD-4190 ≥98%
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| 包装规格: | 5mg 10mg 25mg 50mg 100mg in glass bottle |
| 溶解性: | 溶于DMSO(20mg/ml超声) |
| 产品描述: | 基本信息 产品编号:Z10067 产品名称:ZD-4190 CAS: 413599-62-9 储存条件 粉末 -20℃ 四年 分子式: C19H16BrFN6O2 溶于液体 -80℃ 两年 分子量 459.27 化学名: Solubility (25°C) 体外 DMSO 12mg/mL (26.12mM) Ethanol Insoluble Water Insoluble 体内(现配现用) <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 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。 制备储备液 浓度 溶液体积 质量 1mg 5mg 10mg 1mM 2.1774mL 10.8868mL 21.7737mL 5mM 0.4355mL 2.1774mL 4.3547mL 10mM 0.2177mL 1.0887mL 2.1774mL 生物活性 产品描述 一种有效的,可口服的VEGFR2和EGFR的抑制剂,用于癌症研究。 靶点/IC50 EGFR VEGFR2 体外研究 ZD4190 exhibits cytotoxic activity against the tumor cells. 体内研究 ZD4190 (100mg/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 (50mg/kg, p.o.) prevents outgrowth of residual tumour in a muscle model of minimal residual carcinoma. ZD4190 (12.5-100mg/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. 推荐实验方法(仅供参考) 细胞实验: The cytotoxicity of ZD4190 for PDVC57B cells is established when 104 cells are exposed to 1-10μM ZD4190 for 96 h before MTS solution is added and the optical density measured at 490nm. Cells are also grown to 40% confluence and treated with 1-100μM ZD4190 for 7 days and the cytopathic effect examined by staining with crystal violet 动物实验: ZD4190 is suspended in a 1% (v/v) solution of polyoxyethylene sorbitan mono-oleate in deionized water and administered by oral gavage (0.1mL/10 g body weight). In each experiment, mice are randomized to receive either vehicle or ZD4190, administered once daily using a 1 day (at 0 and 22h) or 7 day (at 0, 24, 48, 72, 96, 120, 144, and 166h) treatment regimen (i.e., daily administration of compound for 1 or 7 days with an additional dose given 2h prior to the end of the treatment period) followed by DCEMRI under terminal anesthesia. |
| 保存条件: | -20℃ |
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