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.
For research use only. We do not sell to patients.
- CAS No.: 3105591-09-8
- Formula: C30H30F3N7O2
- Molecular Weight:577.60
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
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RIOK2 |
In Vitro
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.
Parmacokinetics
In Vivo
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.
- Somatic Cell Culture
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Apoptosis Solutions
- Soft Agar Colony Formation Assay
- MTT Cell Proliferation Assay
- Western Blot
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- Patient-Derived Orthotopic Xenograft (PDOX)
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- Kinase activity and phosphorylation assays
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- Protocol for Cell Counting and Cell Density Analysis
- Patient-Derived Xenograft (PDX)
- Protocol for Kinase activity and phosphorylation assays
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
Chemical Information
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CAS No. 3105591-09-8
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Molecular Weight 577.60
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CQ3196 Related Classifications
HY-175733 Related Classifications
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