Erteberel
Based on 2 publication(s) in Google Scholar
Erteberel (LY500307) is a potent and selective estrogen receptor beta (ERβ) agonist with Ki and EC50 of 1.54 nM and 3.61 nM, respectively. Erteberel has anti-tumor activities.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.49%
- No. CAS: 533884-09-2
- Fòrmula: C18H18O3
- Peso molecular:282.33
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Erteberel
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Actividad biológica
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ERβ 1.54 nM (Ki) |
ERβ 3.61 nM (EC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| PC-3 | EC50 |
0.66 nM
Compound: 7a, SERBA-1
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Activity at ERbeta in PC3 cells by transcription assay
Activity at ERbeta in PC3 cells by transcription assay
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[PMID: 17034120] |
| PC-3 | EC50 |
19.4 nM
Compound: 7a, SERBA-1
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Activity at ERalpha in PC3 cells by transcription assay
Activity at ERalpha in PC3 cells by transcription assay
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[PMID: 17034120] |
Treatment with Erteberel (0.25-10 μM, 72 hours) significantly reduces the proliferation of GBM cells with no activity on normal astrocytes in vitro[2].
Erteberel promotes apoptosis of GBM cells. Erteberel modulated several pathways related to apoptosis, cell cycle, and DNA damage response[2].
Erteberel (0-1000 μM) sensitizes GBM cells to several FDA-approved chemotherapeutic drugs including cisplatin, lomustine and temozolomide[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U87, U251,T98G and normal astrocytes
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Concentration:0.25, 0.5, 1, 2, 4, 6, 8, and 10 μM
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Incubation Time:72 h
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Result:Treatment with Erteberel significantly reduces the viability of various GBM cell lines in a dose-dependent manner. In contrast, viability of normal astrocytes is not affected at the tested doses, suggesting that Erteberel has tumor cell–specific activity[2].
Erteberel (5 mg/Kg body weight/day, oral, 40-50 days) treatment improves the overall survival of tumor-bearing mice in the GL26 syngeneic glioma model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Athymic mice (5-7 weeks) inoculated with OVCAR-3 cells[2]
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Dosage:5mg/Kg body weight
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Administration:Oral, daily for 28 days
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Result:Immunohistochemical analysis reveals that Erteberel treatment significantly reduces the number of proliferation marker Ki-67-positive cells and increases the number of TUNEL-positive apoptotic cells[2].
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 533884-09-2
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Appearance Solid
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Peso molecular 282.33
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Fòrmula C18H18O3
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Color White to light brown
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SMILES
OC1=CC=C2C([C@@](CCC3)([H])[C@@]3([H])[C@H](C4=CC=C(O)C=C4)O2)=C1
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Synonyms
LY500307
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Cell Death Discov
Mitochondrial estrogen receptors alter mitochondrial priming and response to endocrine therapy in breast cancer cells. [Abstract]2021 Jul 22;7(1):189. PMID: 34294688 -
Solvente y solubilidad
DMSO : 100 mg/mL (354.20 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)
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: ≥ 2.5 mg/mL (8.85 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.85 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Zhao L, et al. Pharmacological activation of estrogen receptor beta augments innate immunity to suppress cancer metastasis. Proc Natl Acad Sci U S A. 2018 Apr 17;115(16):E3673-E3681. [Content Brief]
[2]. Sareddy GR, et al. Selective Estrogen Receptor β Agonist LY500307 as a Novel Therapeutic Agent for Glioblastoma. Sci Rep. 2016 Apr 29;6:24185. [Content Brief]
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 | 3.5420 mL | 17.7098 mL | 35.4195 mL | 88.5489 mL |
| 5 mM | 0.7084 mL | 3.5420 mL | 7.0839 mL | 17.7098 mL | |
| 10 mM | 0.3542 mL | 1.7710 mL | 3.5420 mL | 8.8549 mL | |
| 15 mM | 0.2361 mL | 1.1807 mL | 2.3613 mL | 5.9033 mL | |
| 20 mM | 0.1771 mL | 0.8855 mL | 1.7710 mL | 4.4274 mL | |
| 25 mM | 0.1417 mL | 0.7084 mL | 1.4168 mL | 3.5420 mL | |
| 30 mM | 0.1181 mL | 0.5903 mL | 1.1807 mL | 2.9516 mL | |
| 40 mM | 0.0885 mL | 0.4427 mL | 0.8855 mL | 2.2137 mL | |
| 50 mM | 0.0708 mL | 0.3542 mL | 0.7084 mL | 1.7710 mL | |
| 60 mM | 0.0590 mL | 0.2952 mL | 0.5903 mL | 1.4758 mL | |
| 80 mM | 0.0443 mL | 0.2214 mL | 0.4427 mL | 1.1069 mL | |
| 100 mM | 0.0354 mL | 0.1771 mL | 0.3542 mL | 0.8855 mL |
Erteberel Related Classifications
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