CQ3196
CQ3196 is an orally active RIOK2 inhibitor with a Kd of 14 nM. CQ3196 effectively inhibits the ATPase activity of RIOK2, with an IC50 value of 72 nM. CQ3196 inhibits cell proliferation and colony formation in gastric cancer cell lines. CQ3196 induces cell apoptosis in HGC-27 and AGS cells. CQ3196 suppresses downstream signal pathway of RIOK2. CQ3196 reduces phosphorylation of mTOR and AKT. CQ3196 modulates ribosome function and protein synthesis. CQ3196 inhibits tumor growth and can be used for gastric cancer invtro and invivo research.
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- CAS No.: 3105591-09-8
- Formule: C30H30F3N7O2
- Masse moléculaire:577.60
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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RIOK2 |
CQ3196 (72 h) inhibits proliferation of various cancer cells , with IC50s of 0.46 μM (HGC-27), 0.73 μM (AGS), 2.34 μM (KATO III), 2.09 μM (PC-9), 1.56 μM (A549), 1.42 μM (H3255), 0.75 μM (Mia paca-2), 1.75 μM (Hela), 1.46 μM (Molt 4), 0.90 μM (K562) and 1.52 μM (HEK-293)[1].
CQ3196 (30-1000 nM, 14 days) completely inhibits colony formation in HGC-27 and AGS cells at concentrations of 300 nM and above[1].
CQ3196 (30-1000 nM, 48 h) induces early and late-stage apoptosis in HGC-27 and AGS cells in a concentration-dependent manner[1].
CQ3196 (30-1000 nM) significantly decreases the phosphorylation of mTOR and AKT in HGC-27 cells[1].
CQ3196 (30-1000 nM , 48 h) decreases the expression of ribosomal small subunit RPS2[1].
CQ3196 (1 μM , 24 h) down-regulates RPSs, RPLs and some ribosomerelated proteins to modulates ribosome function and protein Synthesis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HGC-27 and AGS cells
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Concentration:30, 100, 300, and 1000 nM
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Incubation Time:48 h
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Result:Induced apoptosis in HGC-27 cells in a concentration-dependent manner, with the apoptotic rate increasing from 6.31 % to 21.12 % at 1000 nM.
Induced apoptosis in AGS cells, with apoptotic cell levels increasing from 6.74 % to 18.2 % at 1000 nM.
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Cell Line:HGC-27 cells
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Concentration:30, 100, 300, and 1000 nM
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Incubation Time:48 h
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Result:Decreased ribosomal small subunit RPS2 expression.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Balb/c-Nude (6 weeks old) injected subcutaneously with HGC-27 cells[1]
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Dosage:25 and 50 mg/kg
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Administration:p.o., every two days for 12 days
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Result:Inhibited tumor growth, with Tumor Growth Inhibition (TGI) of 43.0 % (25 mg/ kg) and 62.3 % (50 mg/kg).
Revealed no significant body weight loss in mice.
Chemical Information
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CAS No. 3105591-09-8
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Masse moléculaire 577.60
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Formule C30H30F3N7O2
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SMILES
COC1=CC=C(C=N1)C2=CC=C3N=C(C4=C(N(N=N4)C5=CC=C(C(C(F)(F)F)=C5)N6CCC(N(C)C)CC6)C3=C2)OC
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CQ3196 Related Classifications
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