PROTAC BET degrader-2
Based on 2 publication(s) in Google Scholar
PROTAC BET degrader-2 is a BET PROTAC degrader. PROTAC BET degrader-2 induces dose-dependent degradation of BRD2, BRD3 and BRD4 proteins in leukemia cells. PROTAC BET degrader-2 inhibits the growth of acute leukemia cells. PROTAC BET degrader-2 can be used for the research of acute leukemia.
(Pink: BET ligand (HY-112429); Blue: Cereblon ligand (HY-43722); Black: linker).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.21%
- CAS. Nr.: 2093388-33-9
- Formel: C41H42N10O6
- Molecular Weight:770.84
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Speicherung:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Publications Citing Use of MedChemExpress (MCE) PROTAC BET degrader-2
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Biologische Aktivität
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BRD2 |
BRD3 |
BRD4 |
Cereblon |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MOLM-13 | IC50 |
72.3 nM
Compound: 25
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Cytotoxicity against human MOLM13 cells assessed as cell growth inhibition after 4 days by WST-8 assay
Cytotoxicity against human MOLM13 cells assessed as cell growth inhibition after 4 days by WST-8 assay
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[PMID: 28339196] |
| RS4-11 | IC50 |
9.6 nM
Compound: 25
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Cytotoxicity against human RS4:11 cells assessed as cell growth inhibition after 4 days by WST-8 assay
Cytotoxicity against human RS4:11 cells assessed as cell growth inhibition after 4 days by WST-8 assay
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[PMID: 28339196] |
PROTAC BET degrader-2 (Compound 25) (4 days) inhibits the proliferation of human acute leukemia cells RS4;11 and MOLM-13, with IC50 values of 9.6 and 72.3 nM[1].
PROTAC BET degrader-2 (10-100 nM; 3 h) induces dose-dependent degradation of BRD2, BRD3 and BRD4 proteins in human acute leukemia cell line RS4;11, and effectively reduces the expression of BRD3 and BRD4 at a concentration of 10 nM after 3 h of incubation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RS4;11 human acute leukemia cells
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Concentration:10, 30 and 100 nM
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Incubation Time:3 h
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Result:Decreased the levels of BRD3 and BRD4 proteins at 10 nM, but was less potent at reducing BRD2 protein levels.
Further reduced BRD2 levels at higher concentrations (30 nM, 100 nM), with all three BET protein levels showing dose-dependent decreases.
Chemical Information
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CAS. Nr. 2093388-33-9
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Appearance Solid
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Molecular Weight 770.84
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Formel C41H42N10O6
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Color Light yellow to yellow
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SMILES
O=C(C1=NC(NC2=CC(C3CC3)=NN2CC)=C4C(NC5=C4C=C(OC)C(C6=C(C)ON=C6C)=C5)=N1)NCCCC7=CC=CC8=C7CN(C(CC9)C(NC9=O)=O)C8=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (2)
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Journal Impact Factor
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Most Recent
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Structure
PROTAC-mediated activation, rather than degradation, of a nuclear receptor reveals complex ligand-receptor interaction network. [Abstract]2024 Dec 5;32(12):2352-2363.e8. PMID: 39389062 -
ACS Pharmacol Transl Sci
General Stepwise Approach to Optimize a TR-FRET Assay for Characterizing the BRD/PROTAC/CRBN Ternary Complex. [Abstract]2021 Feb 26;4(2):941-952. PMID: 33860212
Lösungsmittel & Löslichkeit
DMSO : 50 mg/mL (64.86 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 (stored under nitrogen). 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (3.24 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. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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.
Reinheit & Dokumentation
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Data Sheet (275 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)
Verweise
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 (stored under nitrogen). 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 | 1.2973 mL | 6.4864 mL | 12.9729 mL | 32.4322 mL |
| 5 mM | 0.2595 mL | 1.2973 mL | 2.5946 mL | 6.4864 mL | |
| 10 mM | 0.1297 mL | 0.6486 mL | 1.2973 mL | 3.2432 mL | |
| 15 mM | 0.0865 mL | 0.4324 mL | 0.8649 mL | 2.1621 mL | |
| 20 mM | 0.0649 mL | 0.3243 mL | 0.6486 mL | 1.6216 mL | |
| 25 mM | 0.0519 mL | 0.2595 mL | 0.5189 mL | 1.2973 mL | |
| 30 mM | 0.0432 mL | 0.2162 mL | 0.4324 mL | 1.0811 mL | |
| 40 mM | 0.0324 mL | 0.1622 mL | 0.3243 mL | 0.8108 mL | |
| 50 mM | 0.0259 mL | 0.1297 mL | 0.2595 mL | 0.6486 mL | |
| 60 mM | 0.0216 mL | 0.1081 mL | 0.2162 mL | 0.5405 mL |
PROTAC BET degrader-2 Related Classifications
HY-114228 Related Classifications
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