Lucitanib
作者：齐岳
发布时间：2023-08-25
09:08:38
点击数：
产品名称：Lucitanib
产品描述：
| 产品描述 | Lucitanib 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 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 25 mg/mL (56.37 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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