PROTAC ERα Degrader-1
Based on 1 publication(s) in Google Scholar
PROTAC ERα Degrader-1 comprises an ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Degrader-1 extracts from patent WO2017201449A1, compound P1. PROTAC ERα Degrader-1 is an estrogen receptor-alpha (ERα) degrader.
(Pink: ERα ligand (HY-18719); Blue: VHL ligand (HY-175348); Black: linker).
For research use only. We do not sell to patients.
- Purity: 96.68%
- CAS No.: 2417369-94-7
- Formula: C66H69N7O10
- Molecular Weight:1120.29
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Storage:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) PROTAC ERα Degrader-1
MoreAll PROTACs Isoforms
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Biological Activity
Estrogen receptor-alpha (ERα)[1]
Chemical Information
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CAS No. 2417369-94-7
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Appearance Solid
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Molecular Weight 1120.29
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Formula C66H69N7O10
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Color Off-white to light yellow
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SMILES
OC1=CC=C(/C(C2=CC=C(OCCN(C)C(COCCOCCNC(C3=CC=C(C(N4[C@@H](C)[C@H](NC([C@H](C)NC)=O)C(N(CC5=C(OC)C=CC6=C5C=CC=C6)C7=C4C=C(C#N)C=C7)=O)=O)C=C3)=O)=O)C=C2)=C(C8=CC=CC=C8)\CC)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (1)
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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
Solvent & Solubility
DMSO : 200 mg/mL (178.53 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)
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 90% (20% SBE-β-CD in Saline)
Solubility: 5 mg/mL (4.46 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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.
Protocol
Synthesis of a PROTAC:
i. Attachment of a Linker (L2) to an E3 Ligase Binding Group (E3LB).
ii. Attachment of a protein binding moiety (PB) to an E3LB via a Linker (L2)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (272 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)
References
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 | 0.8926 mL | 4.4631 mL | 8.9263 mL | 22.3156 mL |
| 5 mM | 0.1785 mL | 0.8926 mL | 1.7853 mL | 4.4631 mL | |
| 10 mM | 0.0893 mL | 0.4463 mL | 0.8926 mL | 2.2316 mL | |
| 15 mM | 0.0595 mL | 0.2975 mL | 0.5951 mL | 1.4877 mL | |
| 20 mM | 0.0446 mL | 0.2232 mL | 0.4463 mL | 1.1158 mL | |
| 25 mM | 0.0357 mL | 0.1785 mL | 0.3571 mL | 0.8926 mL | |
| 30 mM | 0.0298 mL | 0.1488 mL | 0.2975 mL | 0.7439 mL | |
| 40 mM | 0.0223 mL | 0.1116 mL | 0.2232 mL | 0.5579 mL | |
| 50 mM | 0.0179 mL | 0.0893 mL | 0.1785 mL | 0.4463 mL | |
| 60 mM | 0.0149 mL | 0.0744 mL | 0.1488 mL | 0.3719 mL | |
| 80 mM | 0.0112 mL | 0.0558 mL | 0.1116 mL | 0.2789 mL | |
| 100 mM | 0.0089 mL | 0.0446 mL | 0.0893 mL | 0.2232 mL |
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