ZEN-2759
Based on 1 Customer Validation
ZEN-2759 is a non-covalent BRD4 inhibitor with IC50 values of 0.23, 0.08, and 0.28 μM for BRD4 (BD1), BRD4 (BD2), and BRD4 (BD1BD2), respectively. ZEN-2759 can be used for cancer research.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.51%
- No. CAS: 1616400-50-0
- Fòrmula: C17H16N2O2
- Peso molecular:280.32
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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
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
[2]|
BRD4 (BD2) 0.08 μM (IC50) |
BRD4 (BD1) 0.23 μM (IC50) |
BRD4(BD1BD2) 0.28 μM (IC50) |
In Vitro
ZEN-2759 disrupts the binding of BRD4 (BD1), BRD4 (BD2), and BRD4 (BD1BD2) to acetylated histone H4 peptide, with target IC50 values of 0.23 μM, 0.08 μM, and 0.28 μM, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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No. CAS 1616400-50-0
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Appearance Solid
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Peso molecular 280.32
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Fòrmula C17H16N2O2
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Color Off-white to light yellow
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SMILES
O=C1C=CC(C2=C(ON=C2C)C)=CN1CC3=CC=CC=C3
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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 : 100 mg/mL (356.74 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.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.92 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 (8.92 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.
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.
Protocolo
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureza y Documentación
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Ficha de datos (275 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 |
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| DMSO | 1 mM | 3.5674 mL | 17.8368 mL | 35.6735 mL | 89.1838 mL |
| 5 mM | 0.7135 mL | 3.5674 mL | 7.1347 mL | 17.8368 mL | |
| 10 mM | 0.3567 mL | 1.7837 mL | 3.5674 mL | 8.9184 mL | |
| 15 mM | 0.2378 mL | 1.1891 mL | 2.3782 mL | 5.9456 mL | |
| 20 mM | 0.1784 mL | 0.8918 mL | 1.7837 mL | 4.4592 mL | |
| 25 mM | 0.1427 mL | 0.7135 mL | 1.4269 mL | 3.5674 mL | |
| 30 mM | 0.1189 mL | 0.5946 mL | 1.1891 mL | 2.9728 mL | |
| 40 mM | 0.0892 mL | 0.4459 mL | 0.8918 mL | 2.2296 mL | |
| 50 mM | 0.0713 mL | 0.3567 mL | 0.7135 mL | 1.7837 mL | |
| 60 mM | 0.0595 mL | 0.2973 mL | 0.5946 mL | 1.4864 mL | |
| 80 mM | 0.0446 mL | 0.2230 mL | 0.4459 mL | 1.1148 mL | |
| 100 mM | 0.0357 mL | 0.1784 mL | 0.3567 mL | 0.8918 mL |
ZEN-2759 Related Classifications
HY-129201 Related Classifications
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