iBRD4-BD1
Based on 1 Customer Validation
iBRD4-BD1 is selective BRD4 bromodomain inhibitor. iBRD4-BD1 has inhibition activity for BRD4 bromodomain with an IC50 value of 12 nM. iBRD4-BD1 can be used for the research of inflammation and oncology.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.77%
- No. CAS: 2839318-17-9
- Fòrmula: C29H30F3N5O
- Peso molecular:521.58
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Almacenamiento:Powder -20°C, 3 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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
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Actividad biológica
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BRD4 |
iBRD4-BD1 has affinity and selectivity for the BET-family BRD4-BD1 with an IC50 value of 12 nM[1].
iBRD4-BD1 has affinity and selectivity for the BET-family BRD4-BD2, BRD3-BD1, BRD3-BD2, BRD2-BD1 and BRD2-BD2 with IC50 values of 16 μM, 1.0 μM , 75 μM , 280 nM and 7.1 μM, respectively[1].
iBRD4-BD1 (0-50 μM; 72 h) has cytotoxicity with an EC50 value of 2.3 μM in MM.1S cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MM.1S cells
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Concentration:0-50 μM
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Incubation Time:72 h
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Result:Showed cytotoxicity with an EC50 value of 2.3 μM in MM.1S cells.
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Cell Line:MM.1S cells
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Concentration:0-300 pM
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Incubation Time:1 h
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Result:Prevented the denaturation of BRD4 in a dose-dependent manner and showed stabilization of BRD4 at concentrations above 3 nM.
Chemical Information
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No. CAS 2839318-17-9
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Appearance Solid
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Peso molecular 521.58
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Fòrmula C29H30F3N5O
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Color White to off-white
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SMILES
FC(F)(C1=CC=C(C2=C(C3=CC=NC(OC4=CC(C(C)C)=CC=C4C)=N3)N(C5CCNCC5)C=N2)C=C1)F
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (191.73 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)
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 (4.79 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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 (4.79 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
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- 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 | 1.9173 mL | 9.5863 mL | 19.1725 mL | 47.9313 mL |
| 5 mM | 0.3835 mL | 1.9173 mL | 3.8345 mL | 9.5863 mL | |
| 10 mM | 0.1917 mL | 0.9586 mL | 1.9173 mL | 4.7931 mL | |
| 15 mM | 0.1278 mL | 0.6391 mL | 1.2782 mL | 3.1954 mL | |
| 20 mM | 0.0959 mL | 0.4793 mL | 0.9586 mL | 2.3966 mL | |
| 25 mM | 0.0767 mL | 0.3835 mL | 0.7669 mL | 1.9173 mL | |
| 30 mM | 0.0639 mL | 0.3195 mL | 0.6391 mL | 1.5977 mL | |
| 40 mM | 0.0479 mL | 0.2397 mL | 0.4793 mL | 1.1983 mL | |
| 50 mM | 0.0383 mL | 0.1917 mL | 0.3835 mL | 0.9586 mL | |
| 60 mM | 0.0320 mL | 0.1598 mL | 0.3195 mL | 0.7989 mL | |
| 80 mM | 0.0240 mL | 0.1198 mL | 0.2397 mL | 0.5991 mL | |
| 100 mM | 0.0192 mL | 0.0959 mL | 0.1917 mL | 0.4793 mL |
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