CQ627
Based on 1 Customer Validation
CQ627 is a molecular glue degrader of right open reading frame kinase 2 (RIOK2). CQ627 inhibits the ATPase activity of RIOK2 in MOLT-4 cells with an IC50 of 98 nM. By recruiting the E3 ubiquitin ligase RNF126, CQ627 promotes RIOK2 ubiquitination and induces its degradation via the ubiquitin-proteasome system (UPS), while inhibiting RIOK2-dependent mTOR/AKT signaling, suppressing cancer cell proliferation, and inducing G2/M cell cycle arrest and apoptosis. CQ627 can be used in studies related to RIOK2-targeted protein degradation and leukemia.
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- Pureza : 98.93%
- No. CAS: 3093767-34-8
- Fòrmula: C36H27F4N7O4
- Peso molecular:697.64
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
[1]|
RIOK2 98 nM (IC50) |
RIOK2 410 nM (DC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MOLT-4 | DC50 |
410 nM
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Induction of RIOK2 degradation in human MOLT4 leukemia cells after 12 h treatment.
Induction of RIOK2 degradation in human MOLT4 leukemia cells after 12 h treatment.
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39721086 |
| MOLT-4 | IC50 |
0.13 μM
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Antiproliferative activity against human MOLT4 leukemia cells assessed after 72 h treatment via CCK8 assay.
Antiproliferative activity against human MOLT4 leukemia cells assessed after 72 h treatment via CCK8 assay.
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39721086 |
| HL-60 | IC50 |
0.34 μM
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Antiproliferative activity against human HL-60 cells assessed after 72 h treatment via CCK8 assay.
Antiproliferative activity against human HL-60 cells assessed after 72 h treatment via CCK8 assay.
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39721086 |
| OCI-Ly3 | IC50 |
0.12 μM
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Antiproliferative activity against human OCILY3 cells assessed after 72 h treatment via CCK8 assay.
Antiproliferative activity against human OCILY3 cells assessed after 72 h treatment via CCK8 assay.
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39721086 |
| U-937 | IC50 |
0.41 μM
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Antiproliferative activity against human U937 cells assessed after 72 h treatment via CCK8 assay.
Antiproliferative activity against human U937 cells assessed after 72 h treatment via CCK8 assay.
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39721086 |
| K562 | IC50 |
1.14 μM
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Antiproliferative activity against human K562 cells assessed after 72 h treatment via CCK8 assay.
Antiproliferative activity against human K562 cells assessed after 72 h treatment via CCK8 assay.
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39721086 |
| ASPC1 | IC50 |
1.13 μM
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Antiproliferative activity against human ASPC-1 cells assessed after 72 h treatment via CCK8 assay.
Antiproliferative activity against human ASPC-1 cells assessed after 72 h treatment via CCK8 assay.
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39721086 |
| A549 | IC50 |
1.06 μM
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Antiproliferative activity against human A549 cells assessed after 72 h treatment via CCK8 assay.
Antiproliferative activity against human A549 cells assessed after 72 h treatment via CCK8 assay.
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39721086 |
| HeLa | IC50 |
0.58 μM
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Antiproliferative activity against human HeLa cells assessed after 72 h treatment via CCK8 assay.
Antiproliferative activity against human HeLa cells assessed after 72 h treatment via CCK8 assay.
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39721086 |
| HEK293 | IC50 |
1.05 μM
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Antiproliferative activity against human HEK293 cells assessed after 72 h treatment via CCK8 assay.
Antiproliferative activity against human HEK293 cells assessed after 72 h treatment via CCK8 assay.
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39721086 |
| NIH3T3 | IC50 |
1.06 μM
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Antiproliferative activity against mouse NIH3T3 cells assessed after 72 h treatment via CCK8 assay.
Antiproliferative activity against mouse NIH3T3 cells assessed after 72 h treatment via CCK8 assay.
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39721086 |
| MRC5 | IC50 |
1.09 μM
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Antiproliferative activity against human MRC5 cells assessed after 72 h treatment via CCK8 assay.
Antiproliferative activity against human MRC5 cells assessed after 72 h treatment via CCK8 assay.
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39721086 |
In Vitro
CQ627 (compound 9s) (12 h) induces dose-dependent degradation of RIOK2 in MOLT-4 cells, with a DC50 of 0.41 μM and a Dmax of 83.4%[1].
CQ627 (1 μM; 4-24 h) reduces RIOK2 protein levels in MOLT-4 cells in a time-dependent manner; a significant reduction is observed at 12 h, with the maximum degradation rate reaching 94.8% at 24 h[1].
CQ627 (1 μM; 12 h) induces RIOK2 degradation in MOLT-4 cells; pretreatment with MG-132 (1 μM; 2 h) or MLN4924 (20 μM; 2 h) restores RIOK2 protein levels, indicating that CQ627-induced RIOK2 degradation depends on the proteasome and Cullin-RING E3 ubiquitin ligase system[1].
CQ627 (67.5-1000 nM; 12 h) inhibits the RIOK2-dependent mTOR/AKT signaling pathway in MOLT-4 cells, and suppresses the activation of mTOR and AKT at 500 nM[1].
CQ627 (1 μM; 12 h) induces RIOK2 degradation in MOLT-4 cells; the RNF126 ligand JP-2-196 (5 μM; 2 h pre-treatment) reverses this degradation effect, while CQ627 increases the ubiquitination level of RIOK2, indicating that CQ627 induces RIOK2 degradation via the ubiquitin-proteasome system (UPS) by recruiting the E3 ubiquitin ligase RNF126[1].
CQ627 (72 h) inhibits the proliferation of various tumor cells, with IC50 values of 0.13, 0.34 and 0.12 μM against MOLT-4, HL-60 and OCILY3 cells, respectively. Moreover, its antiproliferative activity in various tumor cells is approximately 3- to 10-fold higher than that of CQ211[1].
CQ627 (0.5 nM-10 μM; 2 h) inhibits RIOK2 ATPase activity in the ADP-Glo assay, with an IC50 of 0.098 μM[1].
CQ627 (900 nM; 24 h) induces 39.60% G2/M cell cycle arrest in MOLT-4 cells, and induces G2/M phase arrest in a dose-dependent manner[1].
CQ627 (900 nM; 48 h) induces 57.11% apoptosis in MOLT-4 cells and triggers apoptosis in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MOLT4 human leukemia cells
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Concentration:67.5, 125, 250, 500, 1000 nM
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Incubation Time:12 h
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Result:Suppressed the activation of mTOR and AKT at 500 nM, as shown by reduced levels of phosphorylated mTOR and phosphorylated AKT.
Dose-dependently reduced RIOK2 protein levels.
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Cell Line:MOLT4 human leukemia cells
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Concentration:33, 100, 300, 900 nM
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Incubation Time:24 h
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Result:Induced dose-dependent G2/M phase arrest, with 39.60% of cells in G2/M phase after treatment with 900 nM for 24 h.
Dose-dependently reduced protein levels of CDK2 and Cyclin B1.
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Cell Line:MOLT4 human leukemia cells
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Concentration:33, 100, 300, 900 nM
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Incubation Time:48 h
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Result:Induced dose-dependent apoptosis, with 57.11% of cells undergoing apoptosis after treatment with 900 nM for 48 h.
Dose-dependently induced cleavage of PARP and caspase-9, and reduced levels of full-length PARP and caspase-9.
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:CB17-SCID mice (female, 6-8 weeks old, injected subcutaneously with 2 × 107 MOLT-4 cells)[1]
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Dosage:10 mg/kg
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Administration:i.p.; 2 days on/4 days off; three cycles
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Result:Achieved a tumor growth inhibition (TGI) value of 18.6%.
Caused no obvious body weight loss throughout the experiment.
Efficiently degraded RIOK2 protein in tumor tissue.
Chemical Information
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No. CAS 3093767-34-8
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Appearance Solid
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Peso molecular 697.64
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Fòrmula C36H27F4N7O4
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Color White to light yellow
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SMILES
FC1=CC=C(C(/C=C/C(N2CCN(C3=C(C(F)(F)F)C=C(N4N=NC5=C4C6=CC(C7=CC=C(OC)N=C7)=CC=C6NC5=O)C=C3)CC2)=O)=O)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 20 mg/mL (28.67 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (306 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.4334 mL | 7.1670 mL | 14.3340 mL | 35.8351 mL |
| 5 mM | 0.2867 mL | 1.4334 mL | 2.8668 mL | 7.1670 mL | |
| 10 mM | 0.1433 mL | 0.7167 mL | 1.4334 mL | 3.5835 mL | |
| 15 mM | 0.0956 mL | 0.4778 mL | 0.9556 mL | 2.3890 mL | |
| 20 mM | 0.0717 mL | 0.3584 mL | 0.7167 mL | 1.7918 mL | |
| 25 mM | 0.0573 mL | 0.2867 mL | 0.5734 mL | 1.4334 mL |
CQ627 Related Classifications
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