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Art. -Nr.: HY-175733

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CQ3196

CQ3196 is an orally active RIOK2 inhibitor with a K_d 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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 3105591-09-8
Formel: C₃₀H₃₀F₃N₇O₂
Molecular Weight:577.60

Speicherung:

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

Data Sheet (282 KB)

CQ3196 Chemical Structure

CAS. Nr.: 3105591-09-8

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

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.

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

Species	Dose	Route	AUC_0-t	C_max	F	T_1/2	CL
Rat^[1]	10 mg/kg	p.o.	3.5*10^3 μg/L·h	169 ng/mL	23.4 %	/	/
Rat^[1]	2 mg/kg	i.v.	3.0*10^3 μg/L·h	559 ng/mL	/	19.1 h	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.

Chemical Information

CAS. Nr. 3105591-09-8
Molecular Weight 577.60
Formel 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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Ma H, et al. Design, Synthesis and Evaluation of 4-Methoxy-1H-[1,2,3]triazolo[4,5-c]quinolines as Highly Potent and Oral Available RIOK2 Inhibitors. J Med Chem. 2025 Aug 28;68(16):17774-17793. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

MOQ

Minimum order quantity

100 mg

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