Lavendustin B
Based on 1 Customer Validation
Lavendustin B is an inhibitor of HIV-1 integrase interaction with LEDGF/p75 with an IC50 of 94.07 μM. Lavendustin B is an ATP-competitive GLUT1 inhibitor with a Ki of 15 μM. Lavendustin B is also a weak inhibitor of tyrosine kinases.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.02%
- CAS. Nr.: 125697-91-8
- Formel: C21H19NO5
- Molecular Weight:365.38
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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GLUT1 15 μM (Ki) |
HIV-1 integrase interaction with LEDGF/p75 94.07 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | IC50 |
0.5 μg/mL
Compound: 77
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Inhibition of EGFR in human A431 cells
Inhibition of EGFR in human A431 cells
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[PMID: 1479375] |
| A-431 | IC50 |
5 x 10-1μg/mL
Compound: 77
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Inhibition of EGFR in human A431 cells
Inhibition of EGFR in human A431 cells
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[PMID: 1479375] |
In HL-60 cells, Lavendustin B (0-1000 μM) inhibits the uptake of methylglucose, deoxyglucose, and dehydroascorbic acid in human erythrocytes in a dose-dependent manner, with 50% inhibition observed at approximately 10-30 μM. Moreover, increasing concentrations of Lavendustin B inhibited, in a dose-dependent manner, the binding of cytochalasin B to human erythrocyte membranes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 125697-91-8
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Appearance Solid
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Molecular Weight 365.38
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Formel C21H19NO5
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Color White to yellow
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SMILES
O=C(O)C1=CC(N(CC2=CC=CC=C2O)CC3=CC=CC=C3O)=CC=C1O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 50 mg/mL (136.84 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. 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.
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 (6.84 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.84 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Reinheit & Dokumentation
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Data Sheet (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. J C Vera, et al. Direct inhibition of the hexose transporter GLUT1 by tyrosine kinase inhibitors. Biochemistry. 2001 Jan 23;40(3):777-90. [Content Brief]
[2]. Fatima E Agharbaoui, et al. Computational and synthetic approaches for developing Lavendustin B derivatives as allosteric inhibitors of HIV-1 integrase. Eur J Med Chem. 2016 Nov 10;123:673-683. [Content Brief]
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 | 2.7369 mL | 13.6844 mL | 27.3688 mL | 68.4219 mL |
| 5 mM | 0.5474 mL | 2.7369 mL | 5.4738 mL | 13.6844 mL | |
| 10 mM | 0.2737 mL | 1.3684 mL | 2.7369 mL | 6.8422 mL | |
| 15 mM | 0.1825 mL | 0.9123 mL | 1.8246 mL | 4.5615 mL | |
| 20 mM | 0.1368 mL | 0.6842 mL | 1.3684 mL | 3.4211 mL | |
| 25 mM | 0.1095 mL | 0.5474 mL | 1.0948 mL | 2.7369 mL | |
| 30 mM | 0.0912 mL | 0.4561 mL | 0.9123 mL | 2.2807 mL | |
| 40 mM | 0.0684 mL | 0.3421 mL | 0.6842 mL | 1.7105 mL | |
| 50 mM | 0.0547 mL | 0.2737 mL | 0.5474 mL | 1.3684 mL | |
| 60 mM | 0.0456 mL | 0.2281 mL | 0.4561 mL | 1.1404 mL | |
| 80 mM | 0.0342 mL | 0.1711 mL | 0.3421 mL | 0.8553 mL | |
| 100 mM | 0.0274 mL | 0.1368 mL | 0.2737 mL | 0.6842 mL |
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