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Endoxifen (Z-isomer)

CAS No. : 112093-28-4

Biological Activity：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/ERR
Endoxifen 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]

Research Area：Cancer

Targets：Potassium Channel|Estrogen Receptor/ERR

Related Small Molecules:DS20362725;Kv3 modulator 2;LSD1/ER-IN-1;Giredestrant;Avobenzone;Brompheniramine-d6 maleate;Pinacidil;Estriol-d3;Chrysin;AMP-PNP tetralithium;ERRγ Inverse Agonist 1;IK1 inhibitor PA-6;(R)-DPN;VU590;MPP hydrochloride;Domiphen bromide;Mesoridazine benzenesulfonate;GPR30 agonist-1;Diethylstilbestrol;Tetrandrine;20(S)-Ginsenoside Rg3;Endoxifen

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