SF1126

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

SF1126 

SF1126 是双重 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 前体，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

SF1126 Chemical Structure

CAS No. : 936487-67-1

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生物活性

SF1126 is a 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].

IC50 & Target

PI3K/BRD4[1]
体外研究
(In Vitro)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Hep3B, HepG2, SK-Hep1, and Huh7 cells
Concentration: 0 µM; 1 µM; 2 µM; 3 µM; 4 µM; 5 µM; 6 µM
Incubation Time: 48 hours
Result: Resulted in an increased inhibition of HCC proliferation.

Cell Cycle Analysis[1]

Cell Line: Hep3B, HepG2, SK-Hep1, and Huh7 cells
Concentration: 1 µM; 5 µM; 10 µM
Incubation Time: 24 hours
Result: Induced cell-cycle arrest.

Western Blot Analysis[1]

Cell Line: Hep3B, HepG2, SK-Hep1, and Huh7 cells
Concentration: 0.5 µM and 2.5 µM
Incubation Time: Pre-30 mins
Result: Suppressed phosphorylation of AKT, p70S6K, 4EBP1, and ERK in all the cell lines together with sorafenib.

Clinical Trial

分子量

852.84

Formula

C39H48N8O14
CAS 号

936487-67-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [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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