Thalidomide-O-COOH
Based on 2 publication(s) in Google Scholar
Thalidomide-O-COOH (Cereblon ligand 3) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-O-COOH (Cereblon ligand 3) can be connected to the ligand for protein by a linker to form PROTACs.
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- Reinheit : 99.45%
- CAS. Nr.: 1061605-21-7
- Formel: C15H12N2O7
- Molecular Weight:332.27
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Speicherung:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
IC50 & Target
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Cereblon |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
>50 μM
Compound: O-Pom-CO2H
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Cytotoxicity against human HEK293 cells assessed as inhibition of cell viability incubated for 30 mins by cell titer-glo assay
Cytotoxicity against human HEK293 cells assessed as inhibition of cell viability incubated for 30 mins by cell titer-glo assay
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[PMID: 35859867] |
| HEK293 | IC50 |
>50 μM
Compound: O-Pom-CO2H
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Cytotoxicity against human HEK293 cells assessed as inhibition of cell viability incubated for 30 mins in presence of CRBN-tracer by nanoBRET assay
Cytotoxicity against human HEK293 cells assessed as inhibition of cell viability incubated for 30 mins in presence of CRBN-tracer by nanoBRET assay
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[PMID: 35859867] |
| HEK293 | IC50 |
0.83 μM
Compound: O-Pom-CO2H
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Cytotoxicity against permeabilized HEK293 cells assessed as inhibition of cell viability incubated for 30 mins in presence of CRBN-tracer by nanoBRET assay
Cytotoxicity against permeabilized HEK293 cells assessed as inhibition of cell viability incubated for 30 mins in presence of CRBN-tracer by nanoBRET assay
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[PMID: 35859867] |
In Vitro
PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
Chemical Information
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CAS. Nr. 1061605-21-7
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Appearance Solid
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Molecular Weight 332.27
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Formel C15H12N2O7
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Color White to off-white
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SMILES
O=C(N(C(CCC1=O)C(N1)=O)C2=O)C(C2=CC=C3)=C3OCC(O)=O
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Synonyms
Cereblon ligand 3; E3 ligase Ligand 3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°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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J Med Chem
Discovery of Novel Bruton's Tyrosine Kinase PROTACs with Enhanced Selectivity and Cellular Efficacy. [Abstract]2023 Jun 8;66(11):7454-7474. PMID: 37195170 -
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : ≥ 42 mg/mL (126.40 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, 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)
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: ≥ 2.08 mg/mL (6.26 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.26 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Reinheit & Dokumentation
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Data Sheet (276 KB)
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SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Korean - KR (644 KB)
- Portuguese - PT (644 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 | 3.0096 mL | 15.0480 mL | 30.0960 mL | 75.2400 mL |
| 5 mM | 0.6019 mL | 3.0096 mL | 6.0192 mL | 15.0480 mL | |
| 10 mM | 0.3010 mL | 1.5048 mL | 3.0096 mL | 7.5240 mL | |
| 15 mM | 0.2006 mL | 1.0032 mL | 2.0064 mL | 5.0160 mL | |
| 20 mM | 0.1505 mL | 0.7524 mL | 1.5048 mL | 3.7620 mL | |
| 25 mM | 0.1204 mL | 0.6019 mL | 1.2038 mL | 3.0096 mL | |
| 30 mM | 0.1003 mL | 0.5016 mL | 1.0032 mL | 2.5080 mL | |
| 40 mM | 0.0752 mL | 0.3762 mL | 0.7524 mL | 1.8810 mL | |
| 50 mM | 0.0602 mL | 0.3010 mL | 0.6019 mL | 1.5048 mL | |
| 60 mM | 0.0502 mL | 0.2508 mL | 0.5016 mL | 1.2540 mL | |
| 80 mM | 0.0376 mL | 0.1881 mL | 0.3762 mL | 0.9405 mL | |
| 100 mM | 0.0301 mL | 0.1505 mL | 0.3010 mL | 0.7524 mL |
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