Endoxifen hydrochloride

SKU: orb1741201

Description

Endoxifen hydrochloride is the primary active metabolite of Tamoxifen, demonstrating superior estrogen receptor affinity and specificity along with aromatase inhibition. It is a valuable research compound for studying breast cancer mechanisms and evaluating potential therapies in both cellular and animal models.

Research Area

Infectious Disease & Virology, Metabolism Research

Key Properties

• CAS Number: 1197194-41-4
• MW: 409.95
• Purity: 99.95%
• Formula: C₂₅H₂₈ClNO₂
• SMILES: Cl.CC\C(=C(/c1ccc(O)cc1)c1ccc(OCCNC)cc1)c1ccccc1
• Target: Cytochromes P450,Estrogen Receptor/ERR,Parasite,Drug Metabolite
• Solubility: DMSO:55 mg/mL (134.16 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.88 mM);H2O:0.9 mg/mL (2.2 mM)

Bioactivity

• 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.
• 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. 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. 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

, Endoxifenhydrochloride, Endoxifen Hydrochloride, ERR, Estrogen Receptor, estrogen receptor, EstrogenReceptor, Drug Metabolite, DrugMetabolite

Compound Identifiers

PubChem CID

54613017