PROTAC ERα Degrader-2
Based on 1 publication(s) in Google Scholar
PROTAC ERα Degrader-2 is a ERα PROTAC degrader. PROTAC ERα Degrader-2 significantly down-regulates the level of ERα in MCF-7 cells.
(Pink: ERα ligand (HY-43962); Blue: IAP ligand (HY-177389); Black: linker (HY-128833)).
For research use only. We do not sell to patients.
- Purity: 98.92%
- CAS No.: 1351169-29-3
- Formula: C42H61N5O8
- Molecular Weight:763.96
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Storage:
-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
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) PROTAC ERα Degrader-2
MoreAll PROTACs Isoforms
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Biological Activity
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ERα |
cIAP1 |
PROTAC ERα Degrader-2 (Compound 11) (30 μM, 24 h) significantly down-regulates the level of ERα in MCF-7 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 cells
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Concentration:30 μM
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Incubation Time:24 h
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Result:Down-regulated the level of ERα in MCF-7 cells.
Chemical Information
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CAS No. 1351169-29-3
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Appearance Solid
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Molecular Weight 763.96
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Formula C42H61N5O8
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Color White to off-white
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SMILES
C[C@@]12[C@](CC/C2=N\OCC(NCCOCCOCCNC([C@H](CC(C)C)NC([C@@H](O)[C@H](N)CC3=CC=CC=C3)=O)=O)=O)([H])[C@@]4([H])[C@](C5=CC=C(O)C=C5CC4)([H])CC1
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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 (261.79 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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (6.54 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.
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.
Purity & Documentation
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Data Sheet (270 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 |
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| DMSO | 1 mM | 1.3090 mL | 6.5448 mL | 13.0897 mL | 32.7242 mL |
| 5 mM | 0.2618 mL | 1.3090 mL | 2.6179 mL | 6.5448 mL | |
| 10 mM | 0.1309 mL | 0.6545 mL | 1.3090 mL | 3.2724 mL | |
| 15 mM | 0.0873 mL | 0.4363 mL | 0.8726 mL | 2.1816 mL | |
| 20 mM | 0.0654 mL | 0.3272 mL | 0.6545 mL | 1.6362 mL | |
| 25 mM | 0.0524 mL | 0.2618 mL | 0.5236 mL | 1.3090 mL | |
| 30 mM | 0.0436 mL | 0.2182 mL | 0.4363 mL | 1.0908 mL | |
| 40 mM | 0.0327 mL | 0.1636 mL | 0.3272 mL | 0.8181 mL | |
| 50 mM | 0.0262 mL | 0.1309 mL | 0.2618 mL | 0.6545 mL | |
| 60 mM | 0.0218 mL | 0.1091 mL | 0.2182 mL | 0.5454 mL | |
| 80 mM | 0.0164 mL | 0.0818 mL | 0.1636 mL | 0.4091 mL | |
| 100 mM | 0.0131 mL | 0.0654 mL | 0.1309 mL | 0.3272 mL |
PROTAC ERα Degrader-2 Related Classifications
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