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    Drug Metabolite
  3. N-Desmethyltamoxifen hydrochloride

N-Desmethyltamoxifen hydrochloride 

Cat. No.: HY-129099A Purity: 99.61%
Handling Instructions

N-Desmethyltamoxifen hydrochloride 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 hydrochloride 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 hydrochloride Chemical Structure

N-Desmethyltamoxifen hydrochloride Chemical Structure

CAS No. : 15917-65-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 130 In-stock
Estimated Time of Arrival: December 31
5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
10 mg USD 260 In-stock
Estimated Time of Arrival: December 31
25 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 950 In-stock
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100 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

N-Desmethyltamoxifen hydrochloride 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 hydrochloride is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation[1][2][3].

In Vitro

N-desmethyltamoxifen hydrochloride (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 hydrochloride (1.5-10 μM; 114 hours) inhibits growth of MCF 7 human mammary carcinoma cells[2].
N-desmethyltamoxifen hydrochloride, 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

393.95

Formula

C₂₅H₂₈ClNO

CAS No.

15917-65-4

SMILES

CC/C(C1=CC=CC=C1)=C(C2=CC=C(OCCNC)C=C2)\C3=CC=CC=C3.[H]Cl

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 : 83.33 mg/mL (211.52 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5384 mL 12.6920 mL 25.3839 mL
5 mM 0.5077 mL 2.5384 mL 5.0768 mL
10 mM 0.2538 mL 1.2692 mL 2.5384 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.17 mg/mL (5.51 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.17 mg/mL (5.51 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.17 mg/mL (5.51 mM); Clear solution

*All of the co-solvents are provided by MCE.
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Keywords:

N-DesmethyltamoxifenPKCEstrogen Receptor/ERRDrug MetaboliteProtein kinase CmetaboliteantiestrogenceramidemetabolismAMLcellssphingosinephosphorylationcarcinomaInhibitorinhibitorinhibit

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Product name:
N-Desmethyltamoxifen hydrochloride
Cat. No.:
HY-129099A
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