2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. Arzoxifene

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.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Arzoxifene hydrochloride) usually boasts enhanced water solubility and stability.

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Arzoxifene

Arzoxifene Chemische Struktur

CAS. Nr. : 182133-25-1

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Other Forms of Arzoxifene:

Arzoxifene Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Arzoxifene

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen
Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

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Beschreibung

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[1].

IC50 & Target

estrogen[1]
Cellular Effect
Cell Line Type Value Description References
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 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]
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.

Arzoxifene Related Antibodies
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.
Klinische Studie
Molekulargewicht

475.60

Formel

C28H29NO4S
CAS. Nr.
SMILES

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

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
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Arzoxifene Related Classifications

  • Molaritätsrechner

  • Verdünnungsrechner

Die Formel zur Berechnung von Molaritäten

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)

Diese Gleichung wird häufig abgekürzt als: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Arzoxifene182133-25-1LY353381 SERM IIILY 353381LY-353381Estrogen Receptor/ERRorallyactivetriphenylethyleneselectiveestrogenraloxifeneantiestrogeniccancerendometriumInhibitorinhibitorinhibit

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