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SF1126
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SF1126图片
CAS NO:936487-67-1
包装与价格:
包装价格(元)
1mg电议
5mg电议

产品介绍
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)。
Cas No.936487-67-1
别名N2-[1,4-二氧代-4-[[4-(4-氧代-8-苯基-4H-1-苯并吡喃-2-基)吗啉-4-基]甲氧基]丁基]-L-精氨酰甘氨酰-L-ALPHA-天冬氨酰-L-丝氨酸内盐
Canonical SMILESN=C(N)NCCC[C@H](NC(CCC(OC[N+]1(CCOCC1)C(OC(C2=CC=C3)=C3C4=CC=CC=C4)=CC2=O)=O)=O)C(NCC(N[C@@H](CC([O-])=O)C(N[C@@H](CO)C(O)=O)=O)=O)=O
分子式C39H48N8O14
分子量852.84
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.