| 名称 | Lucitanib |
| 描述 | Lucitanib (E-3810) is a novel and potent inhibitor of VEGFR and FGFR, selectively targeting VEGFR1, VEGFR2, VEGFR3, FGFR1, and FGFR2 with IC50 values of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively. |
| 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. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 25 mg/mL (56.37 mM)
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| 关键字 | Fibroblast growth factor receptor | E 3810 | Vascular endothelial growth factor receptor | Inhibitor | FGFR | Lucitanib | E3810 | inhibit | VEGFR |
| 相关产品 | Amlexanox | Nintedanib | Sorafenib | Ferulic Acid | Regorafenib | Formononetin | Pazopanib | Axitinib |
| 相关库 | 经典已知活性库 | 膜蛋白靶向化合物库 | 激酶抑制剂库 | 酪氨酸激酶分子库 | 抗癌临床化合物库 | 药物功能重定位化合物库 | 血管生成库 | 抑制剂库 | 已知活性化合物库 | 抗癌药物库 |
United States
