2. Metabolic Enzyme/Protease Apoptosis
  3. Ser/Thr Kinase Apoptosis
  4. 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.

CQ3196

CQ3196 Chemical Structure

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CQ3196 Related Antibodies

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Description

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[1].

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.

CQ3196 Related Antibodies

Apoptosis Analysis[1]

Cell Line: HGC-27 and AGS cells
Concentration: 30, 100, 300, and 1000 nM
Incubation Time: 48 h
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.

Western Blot Analysis[1]

Cell Line: HGC-27 cells
Concentration: 30, 100, 300, and 1000 nM
Incubation Time: 48 h
Result: Decreased ribosomal small subunit RPS2 expression.
Parmacokinetics[1]
Species Dose Route Indicator value
Rat 10 mg/kg p.o. AUC0-t 3.5*10^3 μg/L·h
Rat 2 mg/kg i.v. AUC0-t 3.0*10^3 μg/L·h
Rat 10 mg/kg p.o. Cmax 169 ng/mL
Rat 2 mg/kg i.v. T1/2 19.1 h
Rat 10 mg/kg p.o. F 23.4 %
Rat 2 mg/kg i.v. Cmax 559 ng/mL
Rat 2 mg/kg i.v. CL 403 mL/h/kg
In Vivo

CQ3196 (25 and 50 mg/kg, p.o., every two days for 12 days) exhibits dose-dependent anti-tumor effects in a HGC-27 gastric cancer xenograft model established in BALB/c nude mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Balb/c-Nude (6 weeks old) injected subcutaneously with HGC-27 cells[1]
Dosage: 25 and 50 mg/kg
Administration: p.o., every two days for 12 days
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.
Molecular Weight

577.60

Formula

C30H30F3N7O2
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
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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CQ3196 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.

Keywords:

CQ3196CQ 3196CQ-3196Ser/Thr KinaseApoptosisProtein Serine-Threonine KinaseTumorRIOK2antiproliferativeHGC-27AGS cellsmTOR AKTRibosomegastric cancercolony formationxenograft modelInhibitorinhibitorinhibit

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