| Name | Endoxifen hydrochloride |
| Description | Endoxifen hydrochloride, a principal active metabolite of Tamoxifen (TAM), exhibits heightened affinity and specificity towards the estrogen receptor and possesses aromatase inhibitory capability. It holds promise for breast cancer research. |
| In vitro | Endoxifen, an hydroxylated metabolite of Tamoxifen, exhibits approximately 100-fold greater potency as an estrogen receptor (ER) antagonist compared to tamoxifen. Furthermore, it indicates that endoxifen, unlike 4-hydroxytamoxifen, induces degradation of ER-alpha in breast cancer cells in addition to its transcriptional effects on the ER.[1]
Endoxifen acts as a potent antiestrogen that promotes the degradation of estrogen receptor α in breast cancer cells. Additionally, it has been demonstrated that endoxifen hinders ERA transcriptional activity and effectively suppresses estrogen-induced proliferation of breast cancer cells, even in the presence of tamoxifen, N-desmethyl-tamoxifen, and 4-hydroxytamoxifen.[2]
Endoxifen exhibits significant growth inhibition at a concentration of 10 μM for all breast cancer cell lines, except for MDAMB-468, which shows moderate inhibition. At a concentration of 10 μM, cytotoxic effects are particularly prominent in MCF7, HS 578T, and BT-549 cells. In contrast, lower concentrations of Endoxifen (0.01-1 μM) result in less significant inhibitory effects compared to 10 μM. However, a concentration of 100 μM of Endoxifen is found to be lethal for all tested cells.[2] |
| In vivo | Endoxifen, when administered orally, is quickly absorbed and readily enters systemic circulation. Administering oral Endoxifen once daily for 28 consecutive days, at dosages of 2, 4, and 8 mg/kg, has demonstrated safety and progressive inhibition of human mammary tumor xenograft growth in female mice.[2] |
| Storage | Shipping with blue ice. |
| Solubility Information | H2O : 0.9 mg/mL (2.2 mM), Sonication and heating to 80℃ are recommended.
DMSO : 55 mg/mL (134.16 mM), Sonication is recommended.
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| Keywords | Endoxifenhydrochloride | Endoxifen Hydrochloride |
| Inhibitors Related | Kaempferol | Mycophenolate Mofetil | CLOZAPINE N-OXIDE | Monomethyl fumarate | Estradiol | Estradiol benzoate | Cholesterol | Isonicotinic acid | Ampyrone | Chrysin | Ethisterone | Nicotinamide N-oxide |
| Related Compound Libraries | Nuclear Receptor Compound Library | Bioactive Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
