GB2095
Based on 1 Customer Validation
GB2095 is an orally active and selective galectin-3 inhibitor. GB2095 shows superior selectivity for both human (KD = 0.036 μM) and mouse galectin-3 (KD = 0.35 μM) over other galectins (such as h-Gal-1/4N/4C/8N/8C/9N/9C and m-galectin-1). GB2095 inhibits tumor growth in syngeneic mouse models of breast and melanoma cancers. GB2095 can be used for breast and melanoma cancer research.
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- Reinheit: 98.92%
- CAS. Nr.: 2574415-75-9
- Formel: C20H17BrClF2N3O4S
- Molecular Weight:548.79
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Speicherung:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
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human Galectin-3 36 nM (Kd) |
mouse Galectin-3 0.35 μM (Kd) |
GB2095 displays a 14-fold selectivity for human galectin-3 over the other tested human galectins (Gal-1, -4N, -4C, -8N, -8C, -9N, -9C) on average, and shows a more pronounced (100-fold) selectivity for mouse galectin-3 over mouse galectin-1[1].
GB2095 shows high permeability and no efflux over a CACO-2 cell monolayer, alongside good hepatic stability in both humans and mice, and exhibits moderate plasma protein binding in both human and mouse plasma[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice implanted with 4T1 cells into the mammary fat pad[1]
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Dosage:30 mg/kg
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Administration:p.o., b.i.d from day 1 to day 25
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Result:Significantly inhibited tumor growth compared to the vehicle group, with a significant reduction in tumor volume observed from day 11.
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Animal Model:C57BL/6N mice implanted with B16-F10 cells into the mammary fat pad[1]
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Dosage:30 mg/kg
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Administration:p.o., b.i.d from day 1 to day 14
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Result:Significantly inhibited tumor growth compared to the vehicle group, with a significant reduction in tumor volume observed from day 10.
Chemical Information
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CAS. Nr. 2574415-75-9
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Appearance Solid
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Molecular Weight 548.79
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Formel C20H17BrClF2N3O4S
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Color White to off-white
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SMILES
O[C@@H]1[C@@H](N2C=C(C3=CC(F)=C(C(F)=C3)Cl)C=N2)[C@H]([C@H](O[C@@H]1SC4=CN=CC(Br)=C4)CO)O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (182.22 mM; Need ultrasonic; 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 (protect from light). 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.56 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
Reinheit & Dokumentation
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Data Sheet (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
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 (protect from light). 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 | 1.8222 mL | 9.1110 mL | 18.2219 mL | 45.5548 mL |
| 5 mM | 0.3644 mL | 1.8222 mL | 3.6444 mL | 9.1110 mL | |
| 10 mM | 0.1822 mL | 0.9111 mL | 1.8222 mL | 4.5555 mL | |
| 15 mM | 0.1215 mL | 0.6074 mL | 1.2148 mL | 3.0370 mL | |
| 20 mM | 0.0911 mL | 0.4555 mL | 0.9111 mL | 2.2777 mL | |
| 25 mM | 0.0729 mL | 0.3644 mL | 0.7289 mL | 1.8222 mL | |
| 30 mM | 0.0607 mL | 0.3037 mL | 0.6074 mL | 1.5185 mL | |
| 40 mM | 0.0456 mL | 0.2278 mL | 0.4555 mL | 1.1389 mL | |
| 50 mM | 0.0364 mL | 0.1822 mL | 0.3644 mL | 0.9111 mL | |
| 60 mM | 0.0304 mL | 0.1518 mL | 0.3037 mL | 0.7592 mL | |
| 80 mM | 0.0228 mL | 0.1139 mL | 0.2278 mL | 0.5694 mL | |
| 100 mM | 0.0182 mL | 0.0911 mL | 0.1822 mL | 0.4555 mL |
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