PROTAC ERα Degrader-6
Based on 1 publication(s) in Google Scholar
PROTAC ERα Degrader-6 is a ERα PROTAC degrader. PROTAC ERα Degrader-6 recruits the VHL E3 ubiquitin ligase to induce the ubiquitination and proteasomal degradation of ERα. PROTAC ERα Degrader-6 can be applied in the research of ERα+ breast cancer.
(Pink: ERα Target protein ligand; Blue: VHL ligand (HY-112078); Black: linker (HY-W129147)).
For research use only. We do not sell to patients.
- Purity : 97.55%
- CAS No.: 3065420-66-5
- Formula: C51H56N6O8S
- Molecular Weight:913.09
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Storage: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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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-6
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Biological Activity
Description
IC50 & Target
[1]|
ERα |
VHL |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
0.11 μM
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Antiproliferative activity against ERα+ MCF-7 cells assessed via CCK-8 cell viability assay after 48 h of incubation.
Antiproliferative activity against ERα+ MCF-7 cells assessed via CCK-8 cell viability assay after 48 h of incubation.
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38320426 |
| DU-145 | IC50 |
> 100 μM
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Antiproliferative activity against DU-145 cells assessed via CCK-8 cell viability assay after 48 h of incubation, with no measurable inhibitory activity observed.
Antiproliferative activity against DU-145 cells assessed via CCK-8 cell viability assay after 48 h of incubation, with no measurable inhibitory activity observed.
|
38320426 |
In Vitro
PROTAC ERα Degrader-6 (Compound A2) (2 h) exhibits a higher relative binding affinity for ERα than for ERβ, with an ERα/ERβ selectivity ratio of 3.79[1].
PROTAC ERα Degrader-6 (5 μM) induces the degradation of ERα in MCF-7 cells[1].
PROTAC ERα Degrader-6 (48 h) effectively inhibits the proliferation of ERα+ MCF-7 breast cancer cells with an IC50 of 0.11 μM, and exhibits no antiproliferative effect on ER-negative DU-145 prostate cancer 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 (ERα+) and DU-145 cells
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Concentration:Serial dilutions
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Incubation Time:48 h
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Result:Showed potent antiproliferative activity against MCF-7 cells with an IC50 value of 0.11 μM.
Exhibited no measurable inhibitory activity against DU-145 cells with an IC50 value > 100 μM.
Chemical Information
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CAS No. 3065420-66-5
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Appearance Solid
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Molecular Weight 913.09
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Formula C51H56N6O8S
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Color Brown to red
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SMILES
O=C(N1C[C@H](O)C[C@H]1C(N[C@@H](C)C2=CC=C(C3=C(C)N=CS3)C=C2)=O)[C@@H](NC(CCCCCCCOC4=C(C=CC(O)=C4)/C=C/C5=C/C(C6=CC(O)=CC=C6O5)=C(C#N)/C#N)=O)C(C)(C)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Nat Commun
ERα blockade in dendritic cells enhances antigen cross-presentation and induces antitumor CD8+ T cell immunity. [Abstract]2026 May 5;17(1):6063. PMID: 42086580
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (54.76 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)
Purity & Documentation
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Data Sheet (285 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. 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 | 1.0952 mL | 5.4759 mL | 10.9518 mL | 27.3796 mL |
| 5 mM | 0.2190 mL | 1.0952 mL | 2.1904 mL | 5.4759 mL | |
| 10 mM | 0.1095 mL | 0.5476 mL | 1.0952 mL | 2.7380 mL | |
| 15 mM | 0.0730 mL | 0.3651 mL | 0.7301 mL | 1.8253 mL | |
| 20 mM | 0.0548 mL | 0.2738 mL | 0.5476 mL | 1.3690 mL | |
| 25 mM | 0.0438 mL | 0.2190 mL | 0.4381 mL | 1.0952 mL | |
| 30 mM | 0.0365 mL | 0.1825 mL | 0.3651 mL | 0.9127 mL | |
| 40 mM | 0.0274 mL | 0.1369 mL | 0.2738 mL | 0.6845 mL | |
| 50 mM | 0.0219 mL | 0.1095 mL | 0.2190 mL | 0.5476 mL |
PROTAC ERα Degrader-6 Related Classifications
HY-157765 Related Classifications
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Keywords
- PROTAC ERα Degrader-6
- 3065420-66-5
- PROTAC ERα Degrader6
- PROTAC ERα Degrader 6
- PROTACs
- Estrogen Receptor/ERR
- estrogen receptor alpha
- ERβ
- proteasomal degradation
- VHL E3 ubiquitin ligase
- ER-negative DU-145 prostate cancer cells
- anti-proliferative activity
- Von Hippel-Lindau
- ERα ubiquitination
- MCF-7 breast cancer cells
- ERα+ breast cancer
- Inhibitor
- inhibitor
- inhibit