dBRD4-BD1
Based on 1 Customer Validation
dBRD4-BD1 is a selective and durable BRD4 degrader with an DC50 value of 280 nM (Dmax=77%). dBRD4-BD1 upregulates BRD2/3 protein level and shows low cytotoxicity than iBRD4-BD1.
(Pink: BRD4 ligand (HY-151594); Blue: Cereblon ligand (HY-103597); Black: linker (HY-W006445)).
For research use only. We do not sell to patients.
- Purity: 98.02%
- CAS No.: 2839318-19-1
- Formula: C50H53F3N8O9
- Molecular Weight:967.00
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Storage: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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
dBRD4-BD1 (64 pM-25 nM; 24 h) degrades BDR4 in a dose-dependent manner[1].
dBRD4-BD1 (5 μM; 0-72 h) increases the protein level of BRD2 and BRD3[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:25, 5, 1, 0.2, 0.04, 0.008, 0.0016 nM and 320 pM, 64 pM
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Incubation Time:24 hours
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Result:Degraded BDR4 in a dose-dependent manner.
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Cell Line:MM.1S cells
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Concentration:5 μM
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Incubation Time:0, 0.5, 1, 2, 4, 8, 12, 24, 30, 36, 48, 72 hours
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Result:Increased the protein amount of BRD2 and BRD3 without decreasing cMyc protein level in 4 hr period.
Chemical Information
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CAS No. 2839318-19-1
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Appearance Solid
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Molecular Weight 967.00
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Formula C50H53F3N8O9
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Color White to light yellow
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SMILES
O=C1NC(C(CC1)N2C(C3=C(C2=O)C(OCC(NCCOCCOCCN4CCC(CC4)N5C=NC(C6=CC=C(C(F)(F)F)C=C6)=C5C7=CC=NC(OC8=CC(C(C)C)=CC=C8C)=N7)=O)=CC=C3)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (103.41 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 (2.59 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.
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.
Purity & Documentation
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Data Sheet (273 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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Handling Instructions (2659 KB)
References
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 | 1.0341 mL | 5.1706 mL | 10.3413 mL | 25.8532 mL |
| 5 mM | 0.2068 mL | 1.0341 mL | 2.0683 mL | 5.1706 mL | |
| 10 mM | 0.1034 mL | 0.5171 mL | 1.0341 mL | 2.5853 mL | |
| 15 mM | 0.0689 mL | 0.3447 mL | 0.6894 mL | 1.7235 mL | |
| 20 mM | 0.0517 mL | 0.2585 mL | 0.5171 mL | 1.2927 mL | |
| 25 mM | 0.0414 mL | 0.2068 mL | 0.4137 mL | 1.0341 mL | |
| 30 mM | 0.0345 mL | 0.1724 mL | 0.3447 mL | 0.8618 mL | |
| 40 mM | 0.0259 mL | 0.1293 mL | 0.2585 mL | 0.6463 mL | |
| 50 mM | 0.0207 mL | 0.1034 mL | 0.2068 mL | 0.5171 mL | |
| 60 mM | 0.0172 mL | 0.0862 mL | 0.1724 mL | 0.4309 mL | |
| 80 mM | 0.0129 mL | 0.0646 mL | 0.1293 mL | 0.3232 mL | |
| 100 mM | 0.0103 mL | 0.0517 mL | 0.1034 mL | 0.2585 mL |
dBRD4-BD1 Related Classifications
HY-151593 Related Classifications
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