SF-1126

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SF-1126 是一种泛 PI3K/BRD4 抑制剂，是 RGDS 缀合的 LY294002 前药，具有增加的溶解度并与特定的整合素结合。

SF-1126?is a pan PI3K/BRD4 inhibitor, RGDS-conjugated LY294002 prodrug that exhibits increased solubility and binds to specific integrins; blocks expression levels of c-Myc in HCC cells, inhibits proliferation, cell cycle, apoptosis, PI3K/AKT/mTOR and Ras/Raf/MAPK pathway; shows significant antitumor activity in vivo.Liver Cancer Phase 1 Clinical.

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.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.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. Cell Viability Assay 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 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 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.

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SF 1126 | SF1126

PI3K/Akt/mTOR signaling

PI3K

PI3K

Cancer

Liver Cancer

936487-67-1

852.84

C39H48N8O14

>98% (HPLC)

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O=C([O-])[C@H](CO)NC([C@H](CC(O)=O)NC(CNC([C@H](CCCNC(N)=N)NC(CCC(OC[N+]1(C2=CC(C3=C(O2)C(C4=CC=CC=C4)=CC=C3)=O)CCOCC1)=O)=O)=O)=O)=O

(4-oxo-4-((4-(4-oxo-8-phenyl-4H-chromen-2-yl)morpholino-4-ium)methoxy)butanoyl)-L-arginylglycyl-L-aspartyl-L-serinate

(-20℃)

With Ice Pack

≥ 2 years