DRB18
Based on 1 publication(s) in Google Scholar
DRB18 is a potent pan-class GLUT inhibitor. DRB18 alters energy-related metabolism in A549 cells by changing the abundance of metabolites in glucose-related pathways. DRB18 can eventually lead to G1/S phase arrest and increase oxidative stress and necrotic cell death. DRB18 has anti-tumor activity.
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- Pureza: 99.58%
- No. CAS: 2863686-81-9
- Fòrmula: C22H23ClN2O2
- Peso molecular:382.88
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) DRB18
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Actividad biológica
GLUT[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H1299 | IC50 |
1.9 μM
Compound: 4v
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Inhibition of glucose uptake in human NCI-H1299 cells incubated for 10 mins followed by L-[3H]2-deoxyglucose and glucose addition and measured after 30 mins by scintillation counting method
Inhibition of glucose uptake in human NCI-H1299 cells incubated for 10 mins followed by L-[3H]2-deoxyglucose and glucose addition and measured after 30 mins by scintillation counting method
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[PMID: 32736210] |
| NCI-H1299 | IC50 |
7 μM
Compound: 4v
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Antiproliferative activity against human NCI-H1299 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human NCI-H1299 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 32736210] |
DRB18 (0-10 μM; 30 min) reduces glucose uptake in GLUT1-4-expressed HEK293 cell lines in a dose-dependent manner with IC50s varying from ~ 900 nM to ~ 9 μM[1].
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DRB18 (5 and 10 μM; 72 hours) causes cell cycle arrest in the G1/S phase transition[1].
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DRB18 (5 and 10 μM; 72 hours) increases ROS levels in A549 cells[1].
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DRB18 (5 and 10 μM; 72 hours) reduces expression of glycosylated GLUT1 and GLUT2-4 in A549 cells 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:GLUT1-4-expressed HEK293 cell lines[1]
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Concentration:0-10 μM
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Incubation Time:30 min
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Result:Reduced glucose uptake in these cell lines in a dose-dependent manner with IC50s varying from ~ 900 nM to ~ 9 μM.
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Cell Line:A549[1]
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Concentration:5 and 10 μM
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Incubation Time:72 hours
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Result:Caused cell cycle arrest in the G1/S phase transition.
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Cell Line:A549[1]
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Concentration:5 and 10 μM
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Incubation Time:72 hours
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Result:Reduced expression of glycosylated GLUT1 and GLUT2-4 in A549 cells in a dose-dependent manner.
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Cell Line:A549[1]
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Concentration:5 and 10 μM
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Incubation Time:72 hours
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Result:Reduced expression of glycosylated GLUT1 and GLUT2-4 in A549 cells in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male NU/J nude mice (3-4 weeks; tumor cell-injected)[1]
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Dosage:10 mg/kg
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Administration:IP; thrice a week for 5 weeks
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Result:The tumors were 44% smaller by volume and 43% smaller by weight, also showed DRB18 decreased expression of GLUT1-4 (Fig. 5f) and reduced proliferative capacity within the xenografted tumor.
Chemical Information
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No. CAS 2863686-81-9
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Appearance Solid
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Peso molecular 382.88
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Fòrmula C22H23ClN2O2
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Color White to yellow
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SMILES
ClC1=CC(NCC2=CC(O)=C(C)C=C2)=C(NCC3=CC=C(C)C(O)=C3)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
Publications (1)
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Journal Impact Factor
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Most Recent
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Biochem Biophys Rep
Dimethyl-2-oxoglutarate but not antioxidants prevents glucose hypometabolism induced neural cell death: implications in the pathogenesis and therapy of Alzheimer's disease. [Abstract]2025 Jul 12:43:102150. PMID: 40688502
Solvente y solubilidad
DMSO : 50 mg/mL (130.59 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 (279 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 | 2.6118 mL | 13.0589 mL | 26.1178 mL | 65.2946 mL |
| 5 mM | 0.5224 mL | 2.6118 mL | 5.2236 mL | 13.0589 mL | |
| 10 mM | 0.2612 mL | 1.3059 mL | 2.6118 mL | 6.5295 mL | |
| 15 mM | 0.1741 mL | 0.8706 mL | 1.7412 mL | 4.3530 mL | |
| 20 mM | 0.1306 mL | 0.6529 mL | 1.3059 mL | 3.2647 mL | |
| 25 mM | 0.1045 mL | 0.5224 mL | 1.0447 mL | 2.6118 mL | |
| 30 mM | 0.0871 mL | 0.4353 mL | 0.8706 mL | 2.1765 mL | |
| 40 mM | 0.0653 mL | 0.3265 mL | 0.6529 mL | 1.6324 mL | |
| 50 mM | 0.0522 mL | 0.2612 mL | 0.5224 mL | 1.3059 mL | |
| 60 mM | 0.0435 mL | 0.2176 mL | 0.4353 mL | 1.0882 mL | |
| 80 mM | 0.0326 mL | 0.1632 mL | 0.3265 mL | 0.8162 mL | |
| 100 mM | 0.0261 mL | 0.1306 mL | 0.2612 mL | 0.6529 mL |
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