BRD4 degrader-3
Based on 1 Customer Validation
BRD4 degrader-3 is a molecular glue degrader targeting BRD4, with binding activity towards the BD1 and BD2 domains of BRD4. BRD4 degrader-3 regulates the activity of BRD4. BRD4 degrader-3 inhibits MYC expression in cancer cells. BRD4 degrader-3 suppresses cell proliferation. BRD4 degrader-3 can be used in research related to acute myeloid leukemia and prostate cancer.
For research use only. We do not sell to patients.
- Purity : 98.41%
- CAS No.: 2413382-30-4
- Formula: C26H29N5O2S
- Molecular Weight:475.61
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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
Biological Activity
Description
IC50 & Target
[1]|
BRD4 BD1 15.5 nM (IC50) |
BRD4 BD2 12.3 nM (IC50) |
In Vitro
BRD4 degrader-3 (6 days) inhibits the proliferation of PC-3-STEAP-1 and EoL-1 cells, with IC50 values of 6.6 nM and 2.2 nM, respectively[1].
BRD4 degrader-3 (4 h) affects MYC mRNA expression in MV-4-11 acute myeloid leukemia cells, with an IC50 of 2.9 nM[1].
BRD4 degrader-3 (Example 1a) binds to the purified BRD4 BD1 and BD2 domains, with IC50 values of 15.5 nM and 12.3 nM, respectively. The IC50 of BRD4 degrader-3 binding to full-length BRD4 is 27.1 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2413382-30-4
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Appearance Solid
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Molecular Weight 475.61
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Formula C26H29N5O2S
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Color White to yellow
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SMILES
O=C(OC(C)(C)C)C[C@H]1C2=NN=C(C)N2C3=C(C(C)=C(C)S3)C(C4=CC=C(C#CCN)C=C4)=N1
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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
In Vitro:
DMSO : 25 mg/mL (52.56 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 (5.26 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 (5.26 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.
Purity & Documentation
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Data Sheet (292 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 |
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| DMSO | 1 mM | 2.1026 mL | 10.5128 mL | 21.0256 mL | 52.5641 mL |
| 5 mM | 0.4205 mL | 2.1026 mL | 4.2051 mL | 10.5128 mL | |
| 10 mM | 0.2103 mL | 1.0513 mL | 2.1026 mL | 5.2564 mL | |
| 15 mM | 0.1402 mL | 0.7009 mL | 1.4017 mL | 3.5043 mL | |
| 20 mM | 0.1051 mL | 0.5256 mL | 1.0513 mL | 2.6282 mL | |
| 25 mM | 0.0841 mL | 0.4205 mL | 0.8410 mL | 2.1026 mL | |
| 30 mM | 0.0701 mL | 0.3504 mL | 0.7009 mL | 1.7521 mL | |
| 40 mM | 0.0526 mL | 0.2628 mL | 0.5256 mL | 1.3141 mL | |
| 50 mM | 0.0421 mL | 0.2103 mL | 0.4205 mL | 1.0513 mL |
BRD4 degrader-3 Related Classifications
HY-136857 Related Classifications
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