Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Famitinib (SHR1020) is a potent orally active multi-targeted kinase inhibitor that effectively inhibits the activity of c-kit, VEGFR-2, and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM, and 6.6 nM, respectively [1]. It demonstrates remarkable antitumor properties in human gastric cancer cells and xenografts, inducing apoptosis [2].
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 14,700 | 6-8周 | ||
50 mg | ¥ 19,200 | 6-8周 | ||
100 mg | ¥ 31,500 | 6-8周 |
产品描述 | Famitinib (SHR1020) is a potent orally active multi-targeted kinase inhibitor that effectively inhibits the activity of c-kit, VEGFR-2, and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM, and 6.6 nM, respectively [1]. It demonstrates remarkable antitumor properties in human gastric cancer cells and xenografts, inducing apoptosis [2]. |
体外活性 | Famitinib inhibits the VEGF-induced proliferation, migration and tubule formation of human umbilical vein endothelial cells, as well as micro-vessel spouting from matrigel-embedded rat aortic rings [1]. Famitinib inhibits cell proliferation by inducing cell cycle arrest at the G2/M phase and causes cell apoptosis in a dose-dependent manner in gastric cancer cell lines. Famitinib (0.6-20.0 μM) inhibits gastric cancer cell growth in a dose-dependent manner [2]. Cell Proliferation Assay [3] Cell Line: Human gastric cancer cells BGC-823 and MGC-803 Concentration: 0, 0.6, 1.25, 2.5, 5.0, 10.0 and 20.0 μM Incubation Time: 24, 48 and 72 hours Result: Inhibited cell growth in a dose-dependent manner. The IC 50 values in BGC-823 and MGC-803 cells were 3.6 and 3.1 μM, respectively. |
体内活性 | Famitinib exerts broad and potent anti-tumor activity, leading to regression or growth arrest of various established xenografts derived from human tumor cell lines [1]. Famitinib significantly slows tumor growth in vivo via inhibition of angiogenesis in BGC-823 xenograft models. Famitinib (50 and 100 mg/kg;gavage) reduces xenograft growth in vivo via inhibition of angiogenesis [2]. Animal Model: 18-20 g female BALB/c athymic nu/nu mice (age, 6–8 weeks) bearing BGC-823 xenografts [4] Dosage: 50 and 100 mg/kg Administration: Gavage, once daily for 3 weeks Result: Both doses exerted a similar inhibitory power, but greater toxicity was observed. Inhibited BGC-823 xenograft growth (tumor volume, 395.2 vs. 2,690.5 mm 3 ), and animal weights were similar between groups (21.6 vs. 18.7 g). |
分子量 | 410.48 |
分子式 | C23H27FN4O2 |
CAS No. | 1044040-56-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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