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

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 proagent, 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 relevant pan and dual first-in-class PI3K/BRD4 inhibitor, has antitumor and anti-angiogenic activity. SF1126 is an RGDS-conjugated LY294002 proagent, 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].

MedChemExpress (MCE) 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
Molecular Weight

852.84

Formula

C39H48N8O14

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

N=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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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SF1126 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
SF1126
Cat. No.:
HY-10220
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