Endoxifen Article
What Is Endoxifen?
Endoxifen, chemically known as 4-hydroxy-N-desmethyltamoxifen, is the primary active metabolite of tamoxifen. Unlike tamoxifen itself—which requires hepatic metabolism via CYP2D6—Endoxifen is already in its pharmacologically active form, making it a compound of significant interest in estrogen receptor research.
In laboratory models, Endoxifen has demonstrated strong binding affinity to estrogen receptors (ERα and ERβ), where it functions as a selective estrogen receptor modulator (SERM). This direct activity has made it a focus of investigation in hormone signaling, receptor regulation, and estrogen-responsive tissue studies.
Mechanism of Action (Research Context)
In vitro and preclinical research suggests that Endoxifen:
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Binds competitively to estrogen receptors
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Inhibits estrogen-mediated gene transcription
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Exhibits tissue-selective estrogen agonist/antagonist behavior
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Demonstrates greater receptor affinity than parent tamoxifen
Because Endoxifen does not require metabolic activation, it is often studied in models where CYP variability is a confounding factor.
Chemical Structure & Properties
Chemical Information
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Chemical Name: 4-hydroxy-N-desmethyltamoxifen
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Common Name: Endoxifen
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Salt Form: Endoxifen Citrate
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Molecular Formula: C₂₅H₂₇NO₂
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Molecular Weight: 373.49 g/mol (free base)
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Chemical Class: Selective Estrogen Receptor Modulator (SERM)
Structurally, Endoxifen retains the triphenylethylene backbone characteristic of tamoxifen derivatives, with hydroxylation contributing to its enhanced receptor affinity and biological activity.
Research Applications
Endoxifen is commonly studied in laboratory environments for:
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Estrogen receptor signaling pathways
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Hormone-responsive cell line assays
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SERM comparative studies
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CYP-independent estrogen modulation models
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Binding affinity and receptor kinetics research
Its consistent activity profile makes it particularly useful in controlled experimental designs.
Handling & Storage (Laboratory Use)
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Store in a cool, dry environment
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Protect from light and moisture
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Handle using appropriate laboratory PPE
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Intended for controlled research environments only
Important Notice
This product is sold strictly for research and laboratory use only.
Not for human consumption, medical use, or veterinary use. All information provided is for educational and scientific reference purposes.
| CAS Number | 110025-28-0 |
| Other Names | 4-hydroxy-N-demethyltamoxifen; 4-hydroxy-N-desmethyltamoxifen; 4-hydroxy-N-desmethyltamoxifen, (Z)-isomer endoxifen; Z-endoxifen |
| IUPAC Name | (E/Z)-4-[1-[4-[2-(Methylamino)ethoxy]phenyl]-2-phenyl-1-buten-1-yl]-phenol |
| Molecular Formula | C25H27NO2 |
| Molecular Weight | 373.49 g/mol |
| Dry-Fill Capsule Concentration | 10mg |
| Liquid Concentration And Solution | 20mg/ml (PEG400,DMSO) |
| Aliquot Concentration And Solution | NA |
