PROTAC ER Degrader-4
Based on 1 Customer Validation
PROTAC ER Degrader-4 is a von Hippel-Lindau-based PROATC estrogen receptor (ER) degrader, binding to ER with an IC50 of 0.8 nM. PROTAC ER Degrader-4 induces ER degradation in MCF-7 cells with an IC50 of 0.3 nM.
(Pink: Estrogen Receptor/ERR ligand (HY-46340); Blue: VHL ligand (HY-112078); Black: linker).
For research use only. We do not sell to patients.
- Purity: 98.78%
- CAS No.: 2361114-15-8
- Formula: C53H67F3N6O8S
- Molecular Weight:1005.19
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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
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
|
VHL |
ER |
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
0.3 nM
Compound: Ex 3
|
Induction of VHL E3 ligase mediated ERalpha degradation in human MCF7 cells assessed as downregulation of ERalpha expression by cell-based immunofluorescence assay
Induction of VHL E3 ligase mediated ERalpha degradation in human MCF7 cells assessed as downregulation of ERalpha expression by cell-based immunofluorescence assay
|
[PMID: 31620216] |
Chemical Information
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CAS No. 2361114-15-8
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Appearance Solid
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Molecular Weight 1005.19
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Formula C53H67F3N6O8S
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Color Light yellow to yellow
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SMILES
CC(C)(F)CN1[C@H](C2=C(C=C(OCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N3[C@@H](C[C@@H](O)C3)C(N[C@H](C4=CC=C(C5=C(N=CS5)C)C=C4)C)=O)=O)=O)C=C2F)F)C6=C(C7=CC=CC=C7N6)C[C@H]1C
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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)
Solvent & Solubility
DMSO : 100 mg/mL (99.48 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)
Purity & Documentation
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Data Sheet (270 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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 | 0.9948 mL | 4.9742 mL | 9.9484 mL | 24.8709 mL |
| 5 mM | 0.1990 mL | 0.9948 mL | 1.9897 mL | 4.9742 mL | |
| 10 mM | 0.0995 mL | 0.4974 mL | 0.9948 mL | 2.4871 mL | |
| 15 mM | 0.0663 mL | 0.3316 mL | 0.6632 mL | 1.6581 mL | |
| 20 mM | 0.0497 mL | 0.2487 mL | 0.4974 mL | 1.2435 mL | |
| 25 mM | 0.0398 mL | 0.1990 mL | 0.3979 mL | 0.9948 mL | |
| 30 mM | 0.0332 mL | 0.1658 mL | 0.3316 mL | 0.8290 mL | |
| 40 mM | 0.0249 mL | 0.1244 mL | 0.2487 mL | 0.6218 mL | |
| 50 mM | 0.0199 mL | 0.0995 mL | 0.1990 mL | 0.4974 mL | |
| 60 mM | 0.0166 mL | 0.0829 mL | 0.1658 mL | 0.4145 mL | |
| 80 mM | 0.0124 mL | 0.0622 mL | 0.1244 mL | 0.3109 mL |
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