ERD-308
Based on 1 publication(s) in Google Scholar
ERD-308 is a potent estrogen receptor (ER) PROTAC degrader. ERD-308 has DC50 values of 0.17 nM and 0.43 nM in MCF-7 and T47D ER+ cells. ERD-308 can inhibit the proliferation of breast cancer cells and exhibits anti-tumor activity.
(Pink: ERα ligand (HY-48027); Blue: VHL ligand (HY-112078); Black: linker (HY-172643)).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.13%
- CAS. Nr.: 2320561-35-9
- Formel: C55H65N5O9S2
- Molecular Weight:1004.26
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Speicherung:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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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Anti-Cancer Compound Library
HY-L025
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Anti-Breast Cancer Compound Library
HY-L074
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Nuclear Receptor Compound Library
HY-L126
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Membrane Receptor-targeted Compound Library
HY-L150
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PROTAC Library
HY-L151
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Bioactive Compound Library Max
HY-L181
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
Publications Citing Use of MedChemExpress (MCE) ERD-308
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Biologische Aktivität
DC50: 0.17 nM (ER in MCF-7 cells), 0.43 nM (ER in T47D ER+ cells)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | DC50 |
0.17 nM
Compound: ERD-308; 32
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Protac activity against VHL/cullin2/ERalpha in human MCF7 cells assessed as ERalpha degradation after 4 hrs by Western blot analysis
Protac activity against VHL/cullin2/ERalpha in human MCF7 cells assessed as ERalpha degradation after 4 hrs by Western blot analysis
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[PMID: 30990042] |
| MCF7 | GI50 |
0.77 nM
Compound: ERD-308; 32
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Inhibition of cell growth in human MCF7 cells after 4 days by wst-8-based colorimetric analysis
Inhibition of cell growth in human MCF7 cells after 4 days by wst-8-based colorimetric analysis
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[PMID: 30990042] |
| T47D | DC50 |
0.43 nM
Compound: ERD-308; 32
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Protac activity against VHL/cullin2/ERalpha in human T47D cells assessed as ERalpha degradation after 4 hrs by Western blot analysis
Protac activity against VHL/cullin2/ERalpha in human T47D cells assessed as ERalpha degradation after 4 hrs by Western blot analysis
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[PMID: 30990042] |
ERD-308 (0.1 nM-1 μM; 8 h-4 days) can inhibit the proliferation of MCF-7 cells (IC50: 0.77 nM) and suppress the mRNA levels of ER-regulated genes pGR and GREB1[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:0.1, 1, 10, 100 and 300 nM
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Incubation Time:8 h
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Result:Suppressed the mRNA levels of pGR and GREB1.
Chemical Information
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CAS. Nr. 2320561-35-9
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Appearance Solid
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Molecular Weight 1004.26
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Formel C55H65N5O9S2
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Color White to yellow
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SMILES
O=C(C1=C(C2=CC=C(O)C=C2)SC3=CC(O)=CC=C13)C4=CC=C(OCCN(CCCCCOCC(N[C@@H](C(C)(C)C)C(N5[C@H](C(N[C@@H](C)C6=CC=C(C7=C(C)N=CS7)C=C6)=O)C[C@@H](O)C5)=O)=O)CC)C=C4
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
Lösungsmittel & Löslichkeit
DMSO : 50 mg/mL (49.79 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 (protect from light). 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 (protect from light). 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)
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: 1.25 mg/mL (1.24 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.25 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 (12.5 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: 1.25 mg/mL (1.24 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.25 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 (12.5 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 (protect from light)
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 (273 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)
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 (protect from light). 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 | 0.9958 mL | 4.9788 mL | 9.9576 mL | 24.8940 mL |
| 5 mM | 0.1992 mL | 0.9958 mL | 1.9915 mL | 4.9788 mL | |
| 10 mM | 0.0996 mL | 0.4979 mL | 0.9958 mL | 2.4894 mL | |
| 15 mM | 0.0664 mL | 0.3319 mL | 0.6638 mL | 1.6596 mL | |
| 20 mM | 0.0498 mL | 0.2489 mL | 0.4979 mL | 1.2447 mL | |
| 25 mM | 0.0398 mL | 0.1992 mL | 0.3983 mL | 0.9958 mL | |
| 30 mM | 0.0332 mL | 0.1660 mL | 0.3319 mL | 0.8298 mL | |
| 40 mM | 0.0249 mL | 0.1245 mL | 0.2489 mL | 0.6223 mL |
ERD-308 Related Classifications
HY-128600 Related Classifications
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