SF1126
Based on 1 Customer Validation
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.
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- CAS No.: 936487-67-1
- Formule: C39H48N8O14
- Masse moléculaire:852.84
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Stockage:
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Activité biologique
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Hep3B, HepG2, SK-Hep1, and Huh7 cells
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Concentration:0 µM; 1 µM; 2 µM; 3 µM; 4 µM; 5 µM; 6 µM
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Incubation Time:48 hours
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Result:Resulted in an increased inhibition of HCC proliferation.
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Cell Line:Hep3B, HepG2, SK-Hep1, and Huh7 cells
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Concentration:1 µM; 5 µM; 10 µM
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Incubation Time:24 hours
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Result:Induced cell-cycle arrest.
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Cell Line:Hep3B, HepG2, SK-Hep1, and Huh7 cells
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Concentration:0.5 µM and 2.5 µM
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Incubation Time:Pre-30 mins
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Result:Suppressed phosphorylation of AKT, p70S6K, 4EBP1, and ERK in all the cell lines together with sorafenib.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 936487-67-1
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Appearance Solid
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Masse moléculaire 852.84
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Formule C39H48N8O14
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Color White to off-white
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Pureté et documentation
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Fiche technique (272 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)