Arzoxifene
Based on 1 publication(s) in Google Scholar
Arzoxifene (LY353381) is an orally active selective estrogen receptor modulator with a fixed ring structure similar to raloxifene. Arzoxifene has minimal side effects with powerful antiestrogenic effects on breast cancer and endometrium, with equally strong favorable estrogenic effects on bone and lipid profile.
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- CAS. Nr.: 182133-25-1
- Formel: C28H29NO4S
- Molecular Weight:475.60
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Biologische Aktivität
estrogen[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
0.3 nM
Compound: 8
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Antagonist activity at estrogen receptor in human MCF7 cells assessed as inhibition of 17beta-estradiol-mediated transcriptional activation after 24 hrs by luciferase reporter gene assay
Antagonist activity at estrogen receptor in human MCF7 cells assessed as inhibition of 17beta-estradiol-mediated transcriptional activation after 24 hrs by luciferase reporter gene assay
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[PMID: 25879485] |
| MCF7 | IC50 |
0.4 μM
Compound: 8
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Cytotoxicity against human MCF7 cells assessed as cell viability after 5 days by CellTiter-Glo assay
Cytotoxicity against human MCF7 cells assessed as cell viability after 5 days by CellTiter-Glo assay
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[PMID: 25879485] |
| MCF7 | EC50 |
0.0002 μM
Compound: 8
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Induction of estrogen receptor-alpha degradation in human MCF7 cells after 4 hrs by in-cell western assay
Induction of estrogen receptor-alpha degradation in human MCF7 cells after 4 hrs by in-cell western assay
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[PMID: 25879485] |
| MCF7 | EC50 |
0.2 nM
Compound: 8
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Induction of estrogen receptor-alpha degradation in human MCF7 cells after 4 hrs by in-cell western assay
Induction of estrogen receptor-alpha degradation in human MCF7 cells after 4 hrs by in-cell western assay
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[PMID: 25879485] |
Arzoxifene reduces estrogen receptor expression in endometrial cancer cell lines (ECC-1)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 182133-25-1
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Molecular Weight 475.60
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Formel C28H29NO4S
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SMILES
OC1=CC=C(C(OC2=CC=C(OCCN3CCCCC3)C=C2)=C(C4=CC=C(OC)C=C4)S5)C5=C1
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Synonyms
LY353381; SERM III
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Viruses
Antiviral Activity of Selective Estrogen Receptor Modulators against Severe Fever with Thrombocytopenia Syndrome Virus In Vitro and In Vivo. [Abstract]2024 Aug 20;16(8):1332. PMID: 39205306
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Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Arzoxifene Related Classifications
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