E7820

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抑制剂描述：

产品名称：E7820

产品别名：见爱必信官网

英文别名：E7820

靶点：Integrin

CAS：289483-69-8

纯度：>98%

外观：见爱必信官网

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

E7820 is a small molecule and aromatic sulfonamide derivative with potential antiangiogenic and antitumor activities. E7820 inhibits angiogenesis by suppressing integrin alpha 2, a cell adhesion molecule expressed on endothelial cells.

溶解性：DMSO: ≥ 33 mg/mL

体外研究：

E7820 treatment inhibits proliferation of HUVEC induced by either bFGF and VEGF in serum-free medium with IC50 values of 0.10 and 0.081 μg/mL, respectively. E7820 also inhibits both bFGF- and VEGF-driven tube formation of HUVEC in this assay. The IC50 values are 0.20 and 0.24 μg/mL, respectively.

体内研究：E7820 (50 mg/kg) with erlotinib has a significantly synergistic antitumor effect in three xenograft models without severe body weight loss. E7820 (50 mg/kg) and erlotinib decrease MVD and enhance apoptosis in tumor-associated endothelial cells, inhibit tumor cell proliferation and enhanced apoptosis, and enhance inhibition of cell proliferation and apoptosis through activation of both intrinsic and extrinsic apoptosis pathways in human NSCLC xenograft models. E7820 shows anti-tumor activity at doses of 50, 100, and 200 mg/kg in the tumor growth and α2-integrin expression experiments. E7820 (50, 100, and 200 mg/kg) inhibits tumor growth in a dose-dependent manner in all s.c. xenograft models. E7820 completely inhibits s.c. tumor growth of LoVo tumor cells and also regresses the tumor mass of KP-1 tumor cells at the dosages of both 100 and 200 mg/kg.

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