Estrogen receptor modulator 1
Based on 1 Customer Validation
Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors.
For research use only. We do not sell to patients.
- Purity: 99.91%
- CAS No.: 63676-22-2
- Formula: C14H10O2S
- Molecular Weight:242.29
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | EC50 |
17 nM
Compound: 3
|
Activation of estrogen response element in HeLa cells stably transfected with human Estrogen receptor beta.
Activation of estrogen response element in HeLa cells stably transfected with human Estrogen receptor beta.
|
[PMID: 11906280] |
| HeLa | EC50 |
50 nM
Compound: 3
|
Activation of estrogen response element in HeLa cells stably transfected with human Estrogen receptor alpha.
Activation of estrogen response element in HeLa cells stably transfected with human Estrogen receptor alpha.
|
[PMID: 11906280] |
| SH-SY5Y | EC50 |
10 nM
Compound: 3
|
Agonist activity in transcriptional activation assay in SH-SY5Y neuroblastoma cells expressing Estrogen receptor beta
Agonist activity in transcriptional activation assay in SH-SY5Y neuroblastoma cells expressing Estrogen receptor beta
|
[PMID: 11906280] |
Estrogen receptor modulator 1 (compound 18) (100 nM; 10 days) inhibits T47D:A18/PKCα and T47D:A18-TAM1 colony formation[2].
Estrogen receptor modulator 1 (100 nM; 9 days) significantly inhibits the growth of MCF-7:5C cell, and induces apoptosis in these cells 6 days[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:T47D:A18/PKCα and T47D:A18-TAM1 cells
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Concentration:100 nM
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Incubation Time:10 days
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Result:Inhibit T47D:A18/PKCα and T47D:A18-TAM1 colony formation.
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Cell Line:MCF-7:5C cells
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Concentration:100 nM
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Incubation Time:9 days
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Result:Significantly inhibited the growth of MCF-7:5C cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:4-6 week old athymic mice (Harlan-Sprague-Dawley)[2]
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Dosage:1.5 mg/animal
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Administration:p.o. ; daily for 2 weeks
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Result:Significantly reduced tumor volume.
Chemical Information
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CAS No. 63676-22-2
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Appearance Solid
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Molecular Weight 242.29
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Formula C14H10O2S
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Color White to off-white
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SMILES
OC1=CC=C(C=C(C2=CC=C(O)C=C2)S3)C3=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (412.73 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 (271 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
[1]. Brogi S, et al. 3D-QSAR using pharmacophore-based alignment and virtual screening for discovery of novel MCF-7 cell line inhibitors. Eur J Med Chem. 2013 Sep;67:344-51. [Content Brief]
[2]. Molloy ME, et al. Novel selective estrogen mimics for the treatment of tamoxifen-resistant breast cancer. Mol Cancer Ther. 2014 Nov;13(11):2515-26. [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 | 4.1273 mL | 20.6364 mL | 41.2729 mL | 103.1821 mL |
| 5 mM | 0.8255 mL | 4.1273 mL | 8.2546 mL | 20.6364 mL | |
| 10 mM | 0.4127 mL | 2.0636 mL | 4.1273 mL | 10.3182 mL | |
| 15 mM | 0.2752 mL | 1.3758 mL | 2.7515 mL | 6.8788 mL | |
| 20 mM | 0.2064 mL | 1.0318 mL | 2.0636 mL | 5.1591 mL | |
| 25 mM | 0.1651 mL | 0.8255 mL | 1.6509 mL | 4.1273 mL | |
| 30 mM | 0.1376 mL | 0.6879 mL | 1.3758 mL | 3.4394 mL | |
| 40 mM | 0.1032 mL | 0.5159 mL | 1.0318 mL | 2.5796 mL | |
| 50 mM | 0.0825 mL | 0.4127 mL | 0.8255 mL | 2.0636 mL | |
| 60 mM | 0.0688 mL | 0.3439 mL | 0.6879 mL | 1.7197 mL | |
| 80 mM | 0.0516 mL | 0.2580 mL | 0.5159 mL | 1.2898 mL | |
| 100 mM | 0.0413 mL | 0.2064 mL | 0.4127 mL | 1.0318 mL |