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Endoxifen Z-isomer hydrochloride

CAS No. : 1032008-74-4

Biological Activity：Endoxifen Z-isomer hydrochloride 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 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 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 concentrations are needed when ERβ is absent.[2]

Research Area：Cancer

Targets：Potassium Channel|Estrogen Receptor/ERR

Related Screening Libraries:Bioactive Compound Library Plus;Membrane Transporter/Ion Channel Compound Library;Anti-Cancer Compound Library;Anti-Alzheimer’s Disease Compound Library;Anti-Breast Cancer Compound Library;Neurodegenerative Disease-related Compound Library;Potassium Channel Compound Library;Nuclear Receptor Compound Library;

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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