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  3. N-Desmethyltamoxifen

N-Desmethyltamoxifen 

Cat. No.: HY-129099
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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.

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[2]

PKC

 

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].

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

357.49

Formula

C₂₅H₂₇NO

CAS No.

31750-48-8

SMILES

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

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Keywords:

N-DesmethyltamoxifenPKCEstrogen Receptor/ERRDrug MetaboliteProtein kinase CmetaboliteantiestrogenceramidemetabolismAMLcellssphingosinephosphorylationcarcinomaInhibitorinhibitorinhibit

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N-Desmethyltamoxifen
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