公告提醒:爱必信所有产品和服务仅用于科学研究,不用于临床应用及其他用途提供产品和服务(也不为任何个人提供产品和服务)! 抑制剂描述: 产品名称:E-3810 产品别名:见爱必信官网 英文别名:E-3810 靶点:VEGFR CAS:1058137-23-7 纯度:>98% 外观:见爱必信官网 保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. 描述: E-3810 is a novel dual inhibitor of the VEGF and FGF receptors. E-3810 has shown strong antiangiogenic properties as well as outstanding antitumor activity in a large number of preclinical models after oral administration, including resistant settings, and has shown high synergy in combination. E-3810 potently and selectively inhibited VEGF receptor (VEGFR)-1, -2, and -3 and FGF receptor (FGFR)-1 and -2 kinases in the nanomolar range. E-3810 exhibited striking antitumor properties at well-tolerated oral doses administered daily in a variety of tumor xenograft models, including early- or late-stage subcutaneous and orthotopic models. In Matrigel plug assays performed in nude mice, E-3810 inhibited basic FGF-induced angiogenesis and reduced blood vessel density as assessed by histologic analysis. E-3810 reduced the distribution of angiogenesis-sensitive contrast agents after only 5 days of treatment. 溶解性:10 mM in DMSO 体外研究: 体内研究:E-3810, at oral dosing of 20 mg/kg for 7 consecutive days, completely inhibits (P. The activity of 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 E-3810, with complete tumor stabilization lasting throughout the 30-day treatment. As in other tumor models, tumors re-grow after withdrawal of E-3810 at a rate similar to control tumors. 产品信息订购:
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