N-DESMETHYLTAMOXIFEN, HYDROCHLORIDE

Product NameN-DESMETHYLTAMOXIFEN, HYDROCHLORIDE
CAS31750-48-8
MFC25H27NO
MW357.49
EINECS
MOL File31750-48-8.mol

Chemical Properties

Boiling point	485.8±33.0 °C(Predicted)
Density	1.047±0.06 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMSO: 72 mg/mL (201.40 mM);Ethanol: 36 mg/mL (100.70 mM)
pka	9.38±0.10(Predicted)
Water Solubility	Water: Insoluble

Usage And Synthesis

Definition

ChEBI: N-Desmethyltamoxifen is a stilbenoid.

Biological Activity

N-Desmethyltamoxifen is the main metabolite of Tamoxifen in the human body. N-Desmethyltamoxifen, a weaker antiestrogen, is a protein kinase C (PKC) inhibitor ten times stronger than Tamoxifen. It is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis and sphingosine phosphorylation.

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).
It inhibits growth of MCF 7 human mammary carcinoma cells.
N-desmethyltamoxifen, resulting from the CYP3A4/5-mediated catalysis of tamoxifen, is the major primary quantitative metabolite of tamoxifen.

Cell Viability Assay

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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

target

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PKC	Estrogen Receptor