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Cat. No.: HY-13556

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Arzoxifene

(Synonyms: LY353381; SERM III)

1 Cited Publications

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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.

For research use only. We do not sell to patients.

CAS No.: 182133-25-1
Formula: C₂₈H₂₉NO₄S
Molecular Weight:475.60

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (269 KB)

Arzoxifene Chemical Structure

CAS No.: 182133-25-1

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

estrogen^[1]

All Estrogen Receptor/ERR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MCF7	IC₅₀	0.3 nM Compound: 8	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	[PMID: 25879485]
MCF7	IC₅₀	0.4 μM Compound: 8	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	[PMID: 25879485]
MCF7	EC₅₀	0.0002 μM Compound: 8	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	[PMID: 25879485]
MCF7	EC₅₀	0.2 nM Compound: 8	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	[PMID: 25879485]

In Vitro

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.

In Vivo

Arzoxifene inhibits MCF-7 breast cancer xenograft growth in oophorectomized athymic mice. Arzoxifene is reported to prevent body weight increase in oophorectomized rats^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 182133-25-1
Molecular Weight 475.60
Formula C₂₈H₂₉NO₄S
SMILES

OC1=CC=C(C(OC2=CC=C(OCCN3CCCCC3)C=C2)=C(C4=CC=C(OC)C=C4)S5)C5=C1
Synonyms

LY353381; SERM III
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (1)

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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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (269 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Jackson LR, et al. Arzoxifene: the evidence for its development in the management of breast cancer. Core Evid. 2008;2(4):251-258. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Purity & Documentation
References

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Arzoxifene

Publications Citing Use of MedChemExpress (MCE) Arzoxifene

All Estrogen Receptor/ERR Isoforms