S80060
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- 公司名稱 上海源葉生物科技有限公司
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- 更新時間 2025/5/15 19:58:11
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- 產(chǎn)品描述： Lucitanib (E-3810) is a novel dual inhibitor of VEGFR and FGFR, potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50s of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively.
- 靶點： VEGFR1：7 nM (IC50)；VEGFR2：25 nM (IC50)；VEGFR3：10 nM (IC50)；FGFR1：17.5 nM (IC50)；FGFR2：82.5 nM (IC50)
- 體內(nèi)研究： Lucitanib (E-3810), at oral dosing of 20 mg/kg for 7 consecutive days, completely inhibits (P<0.01) the="" bfgf="" induced="" angiogenic="" response="" compare="" with="" the="" response="" in="" vehicle-treated="" mice.="" lucitanib="" (e-3810)="" shows="" a="" broad="" spectrum="" of="" activity,="" being="" active="" in="" all="" the="" xenografts="" tested="" (ht29="" colon="" carcinoma,="" a2780="" ovarian="" carcinoma,="" a498,="" sn12k1,="" and="" rxf393="" renal="" carcinomas)="" with="" dose-dependent="" inhibition="" of="" tumor="" growth.="" e-3810="" significantly="" delays="" growth="" during="" treatment,="" but="" tumors="" resume="" their="" growth="" when="" treatment="" is="" suspended;="" in="" a="" few="" cases,="" tumor="" regression="" is="" observed.="" the="" activity="" of="" lucitanib="" (e-3810)="" 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="" (e-3810),="" with="" complete="" tumor="" stabilization="" lasting="" throughout="" the="" 30-day="" treatment.="" as="" in="" other="" tumor="" models,="" tumors="" re-grow="" after="" withdrawal="" of="" lucitanib="" (e-3810)="" at="" a="" rate="" similar="" to="" control="" tumors="">
- 參考文獻：
1. Bello E, et al. E-3810 is a potent dual inhibitor of VEGFR and FGFR that exerts antitumor activity in multiple preclinical models. Cancer Res. 2011 Feb 15;71(4):1396-405. 2. Colzani M, et al. Quantitative chemical proteomics identifies novel targets of the anti-cancer multi-kinase inhibitor E-3810. Mol Cell Proteomics. 2014 Jun;13(6):1495-509. 3. Bello E, et al. The tyrosine kinase inhibitor E-3810 combined with NSC 125973 inhibits the growth of advanced-stage triple-negative breast cancer xenografts. Mol Cancer Ther. 2013 Feb;12(2):131-40
- 溶解度： DMSO : ≥ 20.83 mg/mL (46.97 mM)
- 保存條件： -20℃
- 配置溶液濃度參考：
1mg 5mg 10mg 1 mM 2.255 ml 11.274 ml 22.548 ml 5 mM 0.451 ml 2.255 ml 4.51 ml 10 mM 0.225 ml 1.127 ml 2.255 ml 50 mM 0.045 ml 0.225 ml 0.451 ml
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