1. PI3K/Akt/mTOR
    Apoptosis
  2. PI3K
    Apoptosis
  3. SF1126

SF1126 

Cat. No.: HY-10220
Handling Instructions

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.

For research use only. We do not sell to patients.

SF1126 Chemical Structure

SF1126 Chemical Structure

CAS No. : 936487-67-1

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Description

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].

IC50 & Target

PI3K/BRD4[1]

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].

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.
Molecular Weight

852.84

Formula

C₃₉H₄₈N₈O₁₄

CAS No.

936487-67-1

SMILES

N=C(N)NCCC[[email protected]](NC(CCC(OC[N+]1(CCOCC1)C(OC(C2=CC=C3)=C3C4=CC=CC=C4)=CC2=O)=O)=O)C(NCC(N[[email protected]@H](CC([O-])=O)C(N[[email protected]@H](CO)C(O)=O)=O)=O)=O

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Room temperature in continental US; may vary elsewhere

Storage

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

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