PROTAC BET Degrader-1
Based on 2 publication(s) in Google Scholar
PROTAC BET Degrader-1 is a BRD2/BRD3/BRD4 PROTAC degrader. PROTAC BET Degrader-1 inhibits the growth of acute leukemia cells. PROTAC BET Degrader-1 is applicable to the research of acute leukemia.
(Pink: BRD2 and BRD3 and BRD4 ligand (HY-112429); Blue: Cereblon ligand (HY-42771); Black: linker).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.41%
- No. CAS: 2093386-22-0
- Fòrmula: C44H45N11O9
- Peso molecular:871.90
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) PROTAC BET Degrader-1
MoreVer todos los productos específicos de isoformas PROTACs
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
BRD2 |
BRD3 |
BRD4 |
Cereblon |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MOLM-13 | IC50 |
45.5 nM
Compound: 9
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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 |
4.3 nM
Compound: 9
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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] |
In Vitro
PROTAC BET Degrader-1 (Compound 9) (4 days) potently inhibits the proliferation of RS4;11 and MOLM-13 acute leukemia cells, with IC50 values of 4.3 and 45.5 nM[1].
PROTAC BET Degrader-1 (3-30 nM; 3 hours) effectively degrades BRD2, BRD3 and BRD4 proteins in RS4;11 acute leukemia cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
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Cell Line:human acute leukemia RS4;11 cells
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Concentration:3 nM, 10 nM, 30 nM
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Incubation Time:3 hours
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Result:Effectively decreased the levels of BRD2, BRD3, and BRD4 proteins in RS4;11 cells at concentrations as low as 3-10 nM, whereas the BET inhibitor 8 showed no degradation effect at 100 nM and 300 nM.
Chemical Information
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No. CAS 2093386-22-0
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Appearance Solid
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Peso molecular 871.90
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Fòrmula C44H45N11O9
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Color Light yellow to yellow
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SMILES
CCN1C(NC2=C3C4=CC(OC)=C(C(C(C)=NO5)=C5C)C=C4NC3=NC(C(NCCCCNC(COC6=C(C(N7C(CCC8=O)C(N8)=O)=O)C(C7=O)=CC=C6)=O)=O)=N2)=CC(C9CC9)=N1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
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
Solvente y solubilidad
In Vitro:
DMSO : ≥ 50 mg/mL (57.35 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 1.67 mg/mL (1.92 mM); Clear solution
This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.
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.
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.1469 mL | 5.7346 mL | 11.4692 mL | 28.6730 mL |
| 5 mM | 0.2294 mL | 1.1469 mL | 2.2938 mL | 5.7346 mL | |
| 10 mM | 0.1147 mL | 0.5735 mL | 1.1469 mL | 2.8673 mL | |
| 15 mM | 0.0765 mL | 0.3823 mL | 0.7646 mL | 1.9115 mL | |
| 20 mM | 0.0573 mL | 0.2867 mL | 0.5735 mL | 1.4337 mL | |
| 25 mM | 0.0459 mL | 0.2294 mL | 0.4588 mL | 1.1469 mL | |
| 30 mM | 0.0382 mL | 0.1912 mL | 0.3823 mL | 0.9558 mL | |
| 40 mM | 0.0287 mL | 0.1434 mL | 0.2867 mL | 0.7168 mL | |
| 50 mM | 0.0229 mL | 0.1147 mL | 0.2294 mL | 0.5735 mL |
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