dBET23
Based on 1 Customer Validation
dBET23 is a highly potent and selective BRD4 PROTAC degrader, with a DC50/5h of approximately 50 nM against the BRD4BD1 protein. dBET23 induces the formation of a ternary complex consisting of CRBN, itself, and BRD4BD1, thereby mediating the degradation of BRD4BD1. dBET23 causes downregulation of BRD4 expression in cancer cells. dBET23 can be used for research on malignant tumors.
(Pink: BRD4 ligand (HY-43723); Blue: Cereblon ligand (HY-14658); Black: linker (HY-168726)).
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- Purity: 95.83%
- CAS No.: 1957234-83-1
- 화학식: C43H45ClN8O9S
- 분자량:885.38
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보관:
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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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용액&용해도
- 순도&문서
- References
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Help & FAQs
All PROTACs Isoforms
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Biological Activity
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BRD4 BD1 ~50 nM (DC50) |
dBET23 (145-300 μM; 15 min) mediates the formation of the DDB1ΔB-CRBN-BRD4BD1 complex, in which BRD4BD1 binds to the NTD of CRBN via specific hydrophobic and electrostatic interactions[1].
dBET23 (5 h) potently degrades BRD4BD1 in stable Flip-In 293 reporter cells, with a DC50/5h of approximately 50 nM, but exhibits weak activity against BRD4BD2 (DC50/5h > 1 μM)[1].
dBET23 (1 μM; 5 h) significantly downregulates the expression of BRD4 and other BET family members in MM.1s cells[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. 1957234-83-1
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Appearance Solid
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분자량 885.38
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화학식 C43H45ClN8O9S
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Color Off-white to brown
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SMILES
O=C(OC)C[C@H]1C2=NN=C(C)N2C3=C(C(C)=C(C(NCCCCCCCCNC(COC4=CC=CC(C(N5C(CC6)C(NC6=O)=O)=O)=C4C5=O)=O)=O)S3)C(C7=CC=C(Cl)C=C7)=N1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
용액&용해도
DMSO : 110 mg/mL (124.24 mM; ultrasonic and warming and heat to 60°C; 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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.
순도&문서
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Data Sheet (272 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 (sealed storage, away from moisture and light). 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 | 1.1295 mL | 5.6473 mL | 11.2946 mL | 28.2365 mL |
| 5 mM | 0.2259 mL | 1.1295 mL | 2.2589 mL | 5.6473 mL | |
| 10 mM | 0.1129 mL | 0.5647 mL | 1.1295 mL | 2.8236 mL | |
| 15 mM | 0.0753 mL | 0.3765 mL | 0.7530 mL | 1.8824 mL | |
| 20 mM | 0.0565 mL | 0.2824 mL | 0.5647 mL | 1.4118 mL | |
| 25 mM | 0.0452 mL | 0.2259 mL | 0.4518 mL | 1.1295 mL | |
| 30 mM | 0.0376 mL | 0.1882 mL | 0.3765 mL | 0.9412 mL | |
| 40 mM | 0.0282 mL | 0.1412 mL | 0.2824 mL | 0.7059 mL | |
| 50 mM | 0.0226 mL | 0.1129 mL | 0.2259 mL | 0.5647 mL | |
| 60 mM | 0.0188 mL | 0.0941 mL | 0.1882 mL | 0.4706 mL | |
| 80 mM | 0.0141 mL | 0.0706 mL | 0.1412 mL | 0.3530 mL | |
| 100 mM | 0.0113 mL | 0.0565 mL | 0.1129 mL | 0.2824 mL |
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