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.

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N-Desmethyltamoxifen

N-Desmethyltamoxifen Chemical Structure

CAS No. : 31750-48-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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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.
Appearance

Solid

Color

White to off-white

SMILES

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

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 11.4 mg/mL (31.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7972 mL 13.9860 mL 27.9720 mL
5 mM 0.5594 mL 2.7972 mL 5.5944 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.59%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7972 mL 13.9860 mL 27.9720 mL 69.9301 mL
5 mM 0.5594 mL 2.7972 mL 5.5944 mL 13.9860 mL
10 mM 0.2797 mL 1.3986 mL 2.7972 mL 6.9930 mL
15 mM 0.1865 mL 0.9324 mL 1.8648 mL 4.6620 mL
20 mM 0.1399 mL 0.6993 mL 1.3986 mL 3.4965 mL
25 mM 0.1119 mL 0.5594 mL 1.1189 mL 2.7972 mL
30 mM 0.0932 mL 0.4662 mL 0.9324 mL 2.3310 mL
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  • 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.

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Product Name:
N-Desmethyltamoxifen
Cat. No.:
HY-129099
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