Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Lucitanib (E-3810) 是 VEGFR 和 FGFR 的双重抑制剂,有效和选择性地抑制VEGFR1 (IC50:7 nM),VEGFR2 (IC50:25 nM),VEGFR3 (IC50:10 nM),FGFR1 (IC50:17.5 nM),FGFR2 (IC50:82.5 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 346 | 现货 | ||
2 mg | ¥ 513 | 现货 | ||
5 mg | ¥ 861 | 现货 | ||
10 mg | ¥ 1,420 | 现货 | ||
25 mg | ¥ 2,570 | 现货 | ||
50 mg | ¥ 3,830 | 现货 | ||
100 mg | ¥ 5,490 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 888 | 现货 |
产品描述 | Lucitanib (E-3810) is a novel VEGFR and FGFR inhibitor. It potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 (IC50s: 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively). |
靶点活性 | FGFR1:17.5 nM, FGFR2:82.5 nM, VEGFR1:7 nM, VEGFR3:10 nM, VEGFR2:25 nM |
体外活性 | Lucitanib potently inhibits FGFR2 activity (Ki<0.05 μM), follows by PDGFRα activity (Ki=0.11 μM) and it also potently inhibits VEGF and bFGF-stimulated HUVEC proliferation (IC50: 40 and 50 nM, respectively), which consistent with the inhibitory activity of VEGFR and FGFR auto-phosphorylation. Lucitanib (E-3810) also inhibits CSF-1R (IC50: 5 nM)[1].The Ki values obtained for DDR2, LYN, CARDIAK, CSBP (2), EPHA2, and YES range between 0.26 and 8 μM[2]. |
体内活性 | Lucitanib (20 mg/kg; 7 consecutive days; p.o.) treatment, completely inhibits (P<0.01) the bFGF induced angiogenic response compare with the response in vehicle-treated mice. E-3810 significantly delays growth during treatment, but tumors resume their growth when treatment is suspended; in a few cases, tumor regression is observed[1]. The activity of Lucitanib given at the doses of 15 mg/kg is tested on MDA-MB-231 breast cancer transplanted subcutaneously, at a late stage, when tumor masses reach 350 to 400 mg. This tumor xenograft is very sensitive to Lucitanib , with complete tumor stabilization lasting throughout the 30-day treatment. As in other tumor models, tumors re-grow after withdrawal of Lucitanib at a rate similar to control tumors[3]. Lucitanib displays a broad spectrum of activity, being active in all the xenografts tested (HT29 colon carcinoma, A2780 ovarian carcinoma, A498, SN12K1, and RXF393 renal carcinomas). It has dose-dependent inhibition of tumor growth. |
别名 | E-3810, 德立替尼 |
分子量 | 443.49 |
分子式 | C26H25N3O4 |
CAS No. | 1058137-23-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 25 mg/mL (56.37 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2548 mL | 11.2742 mL | 22.5484 mL | 56.3711 mL |
5 mM | 0.451 mL | 2.2548 mL | 4.5097 mL | 11.2742 mL | |
10 mM | 0.2255 mL | 1.1274 mL | 2.2548 mL | 5.6371 mL | |
20 mM | 0.1127 mL | 0.5637 mL | 1.1274 mL | 2.8186 mL | |
50 mM | 0.0451 mL | 0.2255 mL | 0.451 mL | 1.1274 mL |
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。
Lucitanib 1058137-23-7 Angiogenesis Tyrosine Kinase/Adaptors VEGFR FGFR Fibroblast growth factor receptor E-3810 E 3810 Vascular endothelial growth factor receptor Inhibitor E3810 inhibit 德立替尼 inhibitor