PROTAC Bcl2 degrader-1
Based on 2 publication(s) in Google Scholar
PROTAC Bcl2 degrader-1 (Compound C5) is a PROTAC based on Cereblon ligand, which potently and selectively induces the degradation of Bcl-2 (IC50, 4.94 μM; DC50, 3.0 μM) and Mcl-1 (IC50, 11.81 μM) by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1/Bcl-2 dual inhibitor Nap-1.
(Pink: Bcl-2 Family ligand (HY-129701); Blue: Cereblon ligand (HY-10984); Black: linker (HY-W007545)).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.80%
- No. CAS: 2378801-85-3
- Fòrmula: C45H45BrN6O10S
- Peso molecular:941.84
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Almacenamiento:
-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
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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 Bcl2 degrader-1
MoreVer todos los productos específicos de isoformas PROTACs
More
Actividad biológica
Descripciòn
IC50 & Target
[1]|
Bcl-2 3 μM (DC50) |
Bcl-2 4.94 μM (IC50) |
Mcl-1 11.81 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HeLa | DC50 |
3 μM
Compound: C5
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Induction of CRBN-mediated Bcl-2 degradation in human HeLa cells measured at 12 hrs by Western blot analysis
Induction of CRBN-mediated Bcl-2 degradation in human HeLa cells measured at 12 hrs by Western blot analysis
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[PMID: 31389699] |
In Vitro
Chemical Information
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No. CAS 2378801-85-3
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Appearance Solid
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Peso molecular 941.84
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Fòrmula C45H45BrN6O10S
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Color Light yellow to yellow
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SMILES
O=C(NCCOCCOCCNC1=CC=CC(C(N2C3CCC(NC3=O)=O)=O)=C1C2=O)CCCCC(NCCN4C(C5=C6C(C4=O)=CC=C(C6=CC=C5)SC7=CC=C(C=C7)Br)=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-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
Solvente y solubilidad
In Vitro:
DMSO : 25 mg/mL (26.54 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.
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: ≥ 2.5 mg/mL (2.65 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.
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. * 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.
Pureza y Documentación
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Ficha de datos (271 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 (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 | 1.0618 mL | 5.3088 mL | 10.6175 mL | 26.5438 mL |
| 5 mM | 0.2124 mL | 1.0618 mL | 2.1235 mL | 5.3088 mL | |
| 10 mM | 0.1062 mL | 0.5309 mL | 1.0618 mL | 2.6544 mL | |
| 15 mM | 0.0708 mL | 0.3539 mL | 0.7078 mL | 1.7696 mL | |
| 20 mM | 0.0531 mL | 0.2654 mL | 0.5309 mL | 1.3272 mL | |
| 25 mM | 0.0425 mL | 0.2124 mL | 0.4247 mL | 1.0618 mL |
PROTAC Bcl2 degrader-1 Related Classifications
HY-125876 Related Classifications
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