PROTAC BRD4 Degrader-2
Based on 1 Customer Validation
PROTAC BRD4 Degrader-2 is a PROTAC connected by ligands for Cereblon and BRD4 with an IC50 of 14.2 nM against BRD4 BD1.
(Pink: BRD4 BD1 ligand (HY-150941); Blue: Cereblon ligand (HY-A0003); Black: linker (HY-108369)).
For research use only. We do not sell to patients.
- Purity: 98.30%
- CAS No.: 2185795-53-1
- Formula: C40H39N9O7
- Molecular Weight:757.79
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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
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BRD4 BD1 14.2 nM (IC50) |
Cereblon |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| THP-1 | IC50 |
1.83 μM
Compound: 17
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Antiproliferative activity against human THP1 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo assay
Antiproliferative activity against human THP1 cells assessed as reduction in cell viability incubated for 72 hrs by cell titer glo assay
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[PMID: 31813613] |
PROTAC BRD4 Degrader-2 (Compound 17) inhibits the growth of THP-1 cell line with an IC50 of 1.83±0.016 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human monocyte lymphoma cell line THP-1
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Concentration:72 hours
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Incubation Time:0.81-3.26 μM
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Result:Showd high anti-proliferative potency.
Chemical Information
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CAS No. 2185795-53-1
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Appearance Solid
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Molecular Weight 757.79
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Formula C40H39N9O7
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Color White to light yellow
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SMILES
O=C(NC1=CC=CC2=C1CN(C(CC3)C(NC3=O)=O)C2=O)COCCN4N=NC(CN5C(N(C)C6=C(C=C(C7=C(C)ON=C7C)C=C6)C5C8=CC=CC=C8)=O)=C4
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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 (131.96 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 (3.30 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 (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 | 1.3196 mL | 6.5981 mL | 13.1963 mL | 32.9907 mL |
| 5 mM | 0.2639 mL | 1.3196 mL | 2.6393 mL | 6.5981 mL | |
| 10 mM | 0.1320 mL | 0.6598 mL | 1.3196 mL | 3.2991 mL | |
| 15 mM | 0.0880 mL | 0.4399 mL | 0.8798 mL | 2.1994 mL | |
| 20 mM | 0.0660 mL | 0.3299 mL | 0.6598 mL | 1.6495 mL | |
| 25 mM | 0.0528 mL | 0.2639 mL | 0.5279 mL | 1.3196 mL | |
| 30 mM | 0.0440 mL | 0.2199 mL | 0.4399 mL | 1.0997 mL | |
| 40 mM | 0.0330 mL | 0.1650 mL | 0.3299 mL | 0.8248 mL | |
| 50 mM | 0.0264 mL | 0.1320 mL | 0.2639 mL | 0.6598 mL | |
| 60 mM | 0.0220 mL | 0.1100 mL | 0.2199 mL | 0.5498 mL | |
| 80 mM | 0.0165 mL | 0.0825 mL | 0.1650 mL | 0.4124 mL | |
| 100 mM | 0.0132 mL | 0.0660 mL | 0.1320 mL | 0.3299 mL |
PROTAC BRD4 Degrader-2 Related Classifications
HY-133136 Related Classifications
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