Endoxifen hydrochloride is a estrogen receptor α (ERα) ligand; potent antiestrogen. Metabolite of tamoxifen. Primary metabolite responsible for the effectiveness of tamoxifen in ER-positive breast cancer.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO ≥ 33 mg/mL|
Endoxifen, the active metabolite of tamoxifen, inhibits cloned hERG potassium channels.
Chae YJ, et al. Eur J Pharmacol. 2015 Apr 5;752:1-7. PMID: 25680947.
Endoxifen is a new potent inhibitor of PKC: a potential therapeutic agent for bipolar disorder.
Ali SM, et al. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2665-7. PMID: 20227879.
Orally administered endoxifen is a new therapeutic agent for breast cancer.
Ahmad A, et al. Breast Cancer Res Treat. 2010 Jul;122(2):579-84. PMID: 20052538.
|Related Estrogen Receptor Products|
27-Hydroxycholesterol is a selective estrogen receptor modulator, and it is also an agonist of the liver X receptor.
SAR439859 (Amcenestrant) is an orally active, nonsteroidal and selective degrader of estrogen receptor, it is also a potent antagonist of ER with EC50 of 0.2 nM for ERα degradation.
4-Hydroxytamoxifen is a selective estrogen receptor modulator.
Methylpiperidino pyrazole (MPP) is an agonist for estrogen receptor α and lacks any ligand functionality with estrogen receptor (ER)β.
|Endoxifen E-isomer hydrochloride
Endoxifen E-isomer hydrochloride is a tamoxifen metabolite and potent Selective Estrogen Response Modifier (SERM).
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