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Endoxifen (Z-isomer)

Names

[ CAS No. ]:
112093-28-4

[ Name ]:
Endoxifen (Z-isomer)

[Synonym ]:
Z-Endoxifen
4OHNDtam
4-Hydroxy-N-desmethyltamoxifen
Endoxifen
UNII-46AF8680RC
Endoxifen (Z-isomer)

Biological Activity

[Description]:

Endoxifen Z-isomer is the most important Tamoxifen metabolite responsible for eliciting the anti-estrogenic effects of this drug in breast cancer cells expressing estrogen receptor-alpha (ERα). Endoxifen inhibits hERG tail currents at 50 mV in a concentration-dependent manner with IC50 values of 1.6 μM.IC50 value: 1.6 μM [1]Target: hERG Potassium Channel, Estrogen Receptor/ERREndoxifen Z-isomer is considered a prodrug, since it has a much higher potency for the estrogen receptor than its parent drug. Endoxifen inhibits the hERG channel protein trafficking to the plasma membrane in a concentration-dependent manner with Endoxifen being more potent than Tamoxifen. [1] Endoxifen is also shown to be a more potent inhibitor of estrogen target genes when ERβ is expressed. Additionally, low concentrations of Endoxifen Z-isomer observed in Tamoxifen treated patients with deficient CYP2D6 activity (20 to 40 nM) markedly inhibit estrogen-induced cell proliferation rates in the presence of ERβ, whereas much higher Endoxifen Z-isomer concentrations are needed when ERβ is absent.[2]

[Related Catalog]:

Signaling Pathways >> Others >> Estrogen Receptor/ERR
Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel
Research Areas >> Cancer

[References]

[1]. Chae YJ, et al. Endoxifen, the active metabolite of tamoxifen, inhibits cloned hERG potassium channels. Eur J Pharmacol. 2015 Apr 5;752:1-7.

[2]. Wu X, et al. Estrogen receptor-beta sensitizes breast cancer cells to the anti-estrogenic actions of endoxifen. Breast Cancer Res. 2011 Mar 10;13(2):R27.


[Related Small Molecules]

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Chemical & Physical Properties

[ Density]:
1.099g/cm3

[ Boiling Point ]:
519.327ºC at 760 mmHg

[ Melting Point ]:
127-129°C

[ Molecular Formula ]:
C25H27NO2

[ Molecular Weight ]:
373.48700

[ Flash Point ]:
267.88ºC

[ Exact Mass ]:
373.20400

[ PSA ]:
41.49000

[ LogP ]:
5.75040

[ Vapour Pressure ]:
0mmHg at 25°C

[ Index of Refraction ]:
1.599

[ Storage condition ]:
Amber Vial, -86°C Freezer, Under Inert Atmosphere

Safety Information

[ Symbol ]:

GHS09

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H400

[ Precautionary Statements ]:
P273-P391

[ RIDADR ]:
UN 3077 9 / PGIII

[ RTECS ]:
SL8285000


Related Compounds

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