1. Epigenetics TGF-beta/Smad Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  2. PKC Estrogen Receptor/ERR Drug Metabolite Endogenous Metabolite
  3. N-Desmethyltamoxifen

N-Desmethyltamoxifen is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation.

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

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

N-Desmethyltamoxifen Chemical Structure

N-Desmethyltamoxifen Chemical Structure

CAS No. : 31750-48-8

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Description

N-Desmethyltamoxifen is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation[1][2][3].

IC50 & Target[1][2]

PKC

 

Estrogen Receptor

 

In Vitro

N-desmethyltamoxifen (20-500 ng/ml; 48 hours) has a profound inhibitory effect upon all seven glioma lines (T98G, U87, U138, U373, ALW, AUK, CAS cells)[1].
N-desmethyltamoxifen (1.5-10 μM; 114 hours) inhibits growth of MCF 7 human mammary carcinoma cells[2].
N-desmethyltamoxifen, resulting from the CYP3A4/5-mediated catalysis of tamoxifen, is the major primary quantitative metabolite of tamoxifen[3].

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

Cell Viability Assay[2]

Cell Line: MCF 7 human mammary carcinoma cells
Concentration: 1.5, 2.5, 5, 7.5, 10 μM
Incubation Time: 114 hours
Result: Inhibits growth of MCF 7 human mammary carcinoma cells
Molecular Weight

357.50

Formula

C25H27NO

CAS No.
SMILES

CC/C(C1=CC=CC=C1)=C(C2=CC=C(OCCNC)C=C2)\C3=CC=CC=C3

Structure Classification
Initial Source
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Room temperature in continental US; may vary elsewhere.

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

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    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.

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N-Desmethyltamoxifen
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HY-129099
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