BRD4 degrader-7
Based on 1 Customer Validation
BRD4 degrader-7 (Compound ZZ1) is a CTLH-dependent BRD4 degrader and c-Glue with a DC50 of 489 nM. BRD4 degrader-7 converts to a sulfinic acid derivative inside cells, interacts with the basic pocket of YPEL5, mediates the bridging of BRD4 BD1 to the YPEL5 subunit of the CTLH E3 ubiquitin ligase, and thereby promotes the formation of a ternary complex. BRD4 degrader-7 can be used in research on Ewing's sarcoma and leukemia.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.59%
- Fòrmula: C30H29ClFN5O5S2
- Peso molecular:658.16
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Almacenamiento: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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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
Actividad biológica
Descripciòn
IC50 & Target
[1]|
BRD4 489 nM (DC50) |
CTLH |
In Vitro
BRD4 degrader-7 (ZZ1) (10-10000 nM; 5 h) potently induces proteasome-dependent degradation of BRD4 in Jurkat cells via a non-CRL E3 ligase pathway, with a DC50 of 502 nM[1].
BRD4 degrader-7 (10-10000 nM; 5 h) induces BRD4 degradation in Jurkat cells, with a DC50 of 489 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Appearance Solid
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Peso molecular 658.16
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Fòrmula C30H29ClFN5O5S2
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Color White to off-white
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SMILES
ClC1=CC(C(NC(C=C2)=CC=C2C3=N[C@@H](CC(OC(C)(C)C)=O)C4=NN=C(C)N4C5=C3C(C)=C(C)S5)=O)=CC=C1S(F)(=O)=O
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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 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (151.94 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: ≥ 5 mg/mL (7.60 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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 (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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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, 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 | 1.5194 mL | 7.5969 mL | 15.1939 mL | 37.9847 mL |
| 5 mM | 0.3039 mL | 1.5194 mL | 3.0388 mL | 7.5969 mL | |
| 10 mM | 0.1519 mL | 0.7597 mL | 1.5194 mL | 3.7985 mL | |
| 15 mM | 0.1013 mL | 0.5065 mL | 1.0129 mL | 2.5323 mL | |
| 20 mM | 0.0760 mL | 0.3798 mL | 0.7597 mL | 1.8992 mL | |
| 25 mM | 0.0608 mL | 0.3039 mL | 0.6078 mL | 1.5194 mL | |
| 30 mM | 0.0506 mL | 0.2532 mL | 0.5065 mL | 1.2662 mL | |
| 40 mM | 0.0380 mL | 0.1899 mL | 0.3798 mL | 0.9496 mL | |
| 50 mM | 0.0304 mL | 0.1519 mL | 0.3039 mL | 0.7597 mL | |
| 60 mM | 0.0253 mL | 0.1266 mL | 0.2532 mL | 0.6331 mL | |
| 80 mM | 0.0190 mL | 0.0950 mL | 0.1899 mL | 0.4748 mL | |
| 100 mM | 0.0152 mL | 0.0760 mL | 0.1519 mL | 0.3798 mL |
BRD4 degrader-7 Related Classifications
HY-183077 Related Classifications
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