GLUT4-IN-2
Based on 1 Customer Validation
GLUT4-IN-2 is a potent and selective GLUT4 inhibitor with IC50s of 11.4 µM and 6.8 µM for GLUT1 and GLUT4, respectively. GLUT4-IN-2 induces cell apoptosis and cell cycle arrest at G0/G1phase. GLUT4-IN-2 shows potent antitumor activity.
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- Pureté : 99.17%
- CAS No.: 2454113-83-6
- Formule: C17H11N3O4S2
- Masse moléculaire:385.42
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
GLUT1 11.4 μM (IC50) |
GLUT4 6.8 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CCRF-CEM | CC50 |
1.7 μM
Compound: F18
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Cytotoxicity against human CCRF-CEM cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis
Cytotoxicity against human CCRF-CEM cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis
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[PMID: 32634629] |
| HS27 | CC50 |
44 μM
Compound: F18
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Cytotoxicity against human HS27 cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis
Cytotoxicity against human HS27 cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis
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[PMID: 32634629] |
| K562 | CC50 |
91.9 μM
Compound: F18
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Cytotoxicity against human K562 cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis
Cytotoxicity against human K562 cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis
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[PMID: 32634629] |
| KCL-22 | CC50 |
15.3 μM
Compound: F18
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Cytotoxicity against human KCL-22 cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis
Cytotoxicity against human KCL-22 cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis
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[PMID: 32634629] |
| MDA-MB-231 | CC50 |
45.1 μM
Compound: F18
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Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 48 hrs by Hoechst 33342/propidium iodide staining based imaging analysis
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[PMID: 32634629] |
In Vitro
GLUT4-IN-2 (compound F18) induces cell apoptosis and ell cycle arrest at G0/G1phase in CME cells[1].
GLUT4-IN-2 (10 µM; 6 h) decreases the expression of mTOR and CDK2, but increases the expression of GRP78, and cleaved caspase 3 proteins [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CME, K562, KCL-22, MB-231, HS-27 cells
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Concentration:1-100 µM
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Incubation Time:48 h
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Result:Showed potent cytotoxicity with cytotoxic concentration 50% (CC50) of 1.7, 91.9, 15.3, 45.1, 44.0 µM for CME, K562, KCL-22, MB-231, HS-27 cells, respectively.
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Cell Line:CEM cells
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Concentration:1.7 µM
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Incubation Time:24 h
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Result:Induced cell apoptosis with the percentage of apoptotic cells in the late and early apoptosis region was 55.87% and 1.38%, respectively.
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Cell Line:CEM cells
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Concentration:10, 25, 50 µM
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Incubation Time:72 h
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Result:Induced cell cycle arrest at G0/G1phase in a dose-dependent manner.
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Cell Line:CEM cells
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Concentration:10 µM
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Incubation Time:6 h
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Result:Decreased the phosphorylation of mTOR and CDK2 proteins and increased the expression of GRP78, and cleaved caspase 3.
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Cell Line:CEM cells
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Concentration:2.5-100 µM
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Incubation Time:48 h
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Result:Showed cytotoxicity with the IC50s of 1.7, 187.2 µM for CEM, WBCs cells respectively.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:8–10 weeks, SCID mice (CEM xenograft tumor) [1]
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Dosage:50 mg/kg
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Administration:I.p.; administered on day 1-5, 8-12, 15-18
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Result:Showed potent antitumor activity in vivo.
Chemical Information
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CAS No. 2454113-83-6
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Appearance Solid
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Masse moléculaire 385.42
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Formule C17H11N3O4S2
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Color Off-white to light yellow
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SMILES
O=C(NC1=NC2=CC=CC=C2S1)CN(C/3=O)C(SC3=C\C4=CC=CO4)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (259.46 mM; ultrasonic and warming and heat to 80°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)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (278 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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Instruction de manipulation (2659 KB)
Références
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 | 2.5946 mL | 12.9729 mL | 25.9457 mL | 64.8643 mL |
| 5 mM | 0.5189 mL | 2.5946 mL | 5.1891 mL | 12.9729 mL | |
| 10 mM | 0.2595 mL | 1.2973 mL | 2.5946 mL | 6.4864 mL | |
| 15 mM | 0.1730 mL | 0.8649 mL | 1.7297 mL | 4.3243 mL | |
| 20 mM | 0.1297 mL | 0.6486 mL | 1.2973 mL | 3.2432 mL | |
| 25 mM | 0.1038 mL | 0.5189 mL | 1.0378 mL | 2.5946 mL | |
| 30 mM | 0.0865 mL | 0.4324 mL | 0.8649 mL | 2.1621 mL | |
| 40 mM | 0.0649 mL | 0.3243 mL | 0.6486 mL | 1.6216 mL | |
| 50 mM | 0.0519 mL | 0.2595 mL | 0.5189 mL | 1.2973 mL | |
| 60 mM | 0.0432 mL | 0.2162 mL | 0.4324 mL | 1.0811 mL | |
| 80 mM | 0.0324 mL | 0.1622 mL | 0.3243 mL | 0.8108 mL | |
| 100 mM | 0.0259 mL | 0.1297 mL | 0.2595 mL | 0.6486 mL |
GLUT4-IN-2 Related Classifications
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