SF1126 是临床相关的双重 PI3K/BRD4 泛抑制剂，具有抗肿瘤和抗血管生成活性。SF1126 是 RGDS-缀合的 LY294002 前药，其设计为表现出增加的溶解度并与肿瘤区室内的特定整联蛋白结合。SF1126 诱导细胞凋亡 (apoptosis)。
SF1126 is a clinically relevant pan and dual first-in-class PI3K/BRD4 inhibitor, has antitumor and anti-angiogenic activity. SF1126 is an RGDS-conjugated LY294002 prodrug, which is designed to exhibit increased solubility and bind to specific integrins within the tumor compartment. SF1126 induces cell apoptosis[1]. PI3K/BRD4[1]
SF1126 (0-6 µM; 48 hours) inhibits Hep3B, HepG2, SK-Hep1, and Huh7 cells proliferation with IC50s of 5.05, 6.89, 3.14, and 2.14 µM, respectively[1].SF1126 (1-10 µM; 24 hours) results in cell-cycle arrest with a proportional increase in G0-G1 and a decrease in the number of cells in the S-phase in Hep 3B, Hep G2, SK-Hep1, and Huh7 cells[1].SF1126 (0.5-2.5 µM; pre-30 minutes) and sorafenib suggests that combined treatment of SF1126 and sorafenib blocks multiple key enzymes in PI3K/AKT/mTOR and Ras/Raf/MAPK pathway[1]. Cell Viability Assay[1] Cell Line: Hep3B, HepG2, SK-Hep1, and Huh7 cells
[1]. Garlich JR, et al. A vascular targeted pan phosphoinositide 3-kinase inhibitor prodrug, SF1126, with antitumor and antiangiogenic activity. Cancer Res. 2008 Jan 1;68(1):206-15.
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