| Name | Endoxifen Z-isomer hydrochloride |
| Description | Endoxifen Z-isomer hydrochloride (Endoxifen HCl) is the active metabolite of Tamoxifen, which is an effective and selective estrogen receptor antagonist. |
| Cell Research | MCF7 and Ishikawa cells are grown in 10% triple charcoal-stripped serum-containing medium for 3 d. The cells are then plated at a density of 2,000 cells per well in 96-well tissue culture plates and treated as indicated every 48 h. Cell proliferation assays are conducted 8 days after the first treatment using a CellTiter-Glo Luminescent Cell Viability kit according to the manufacturer's protocol.(Only for Reference) |
| In vitro | Endoxifen shows anti-estrogenic effects, and decreases the E2-induced PR expression in MCF-7 cells. [1] Endoxifen also blocks ER-alpha transcriptional activity and inhibits estrogen-induced breast cancer cell proliferation. [2] In MCF7, HS 578T, and BT-549 cells, Endoxifen significantly inhibits cell proliferation. [3] Endoxifen also exhibits four-fold higher inhibition on PKC activity compared to tamoxifen. [4] Endoxifen inhibits the hERG current by preferentially interacting with the activated states of cloned hERG potassium channels with IC50 of 1.6 μM. [5] |
| In vivo | In vivo, Endoxifen (8 mg/kg, ) inhibits growth of MCF-7 human mammary tumor xenografts in mice, showing more potency than Tamoxifen. [3] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O : <1 mg/mL
Ethanol : 69 mg/mL (168.31 mM), Sonication is recommended.
DMSO : 69 mg/mL (168.31 mM), Sonication is recommended.
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| Keywords | progestogenReceptor | progestogen Receptor | PotassiumChannel | Potassium Channel | KcsA | Inhibitor | inhibit | hERG | EstrogenReceptor | Estrogen Receptor/ERR | Estrogen Receptor | ERR | ER | Endoxifen Z-isomer Hydrochloride | Endoxifen Zisomer hydrochloride | Endoxifen Z-isomer | Endoxifen Z isomer hydrochloride |
| Inhibitors Related | Minoxidil sulfate | Tamoxifen | Tannic acid | Mifepristone | Estradiol | Hydrochlorothiazide | Astragaloside IV | Bisphenol B | Melatonin | Ethisterone | Chlorzoxazone | Indapamide |
United States
