Molecular Weight(MW): 409.95
Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.
Purity & Quality Control
Choose Selective Estrogen/progestogen Receptor Inhibitors
|Description||Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.|
Endoxifen shows anti-estrogenic effects, and decreases the E2-induced PR expression in MCF-7 cells.  Endoxifen also blocks ER-alpha transcriptional activity and inhibits estrogen-induced breast cancer cell proliferation.  In MCF7, HS 578T, and BT-549 cells, Endoxifen significantly inhibits cell proliferation.  Endoxifen also exhibits four-fold higher inhibition on PKC activity compared to tamoxifen.  Endoxifen inhibits the hERG current by preferentially interacting with the activated states of cloned hERG potassium channels with IC50 of 1.6 μM. 
|In vivo||In vivo, Endoxifen (8 mg/kg, ) inhibits growth of MCF-7 human mammary tumor xenografts in mice, showing more potency than Tamoxifen. |
-  Lim YC, et al. Cancer Chemother Pharmacol. 2005, 55(5), 471-478.
-  Wu X, et al. Cancer Res. 2009, 69(5), 1722-1727.
-  Ahmad A, et al. Breast Cancer Res Treat. 2010, 122(2), 579-584.
|In vitro||DMSO||74 mg/mL (180.5 mM)|
|Ethanol||74 mg/mL (180.5 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03582865||Not yet recruiting||Drug: Tamoxifen 20 mg||Breast Cancer||Assiut University||September 1 2019||--|
|NCT03504631||Recruiting||Other: No intervention||Breast Cancer Female||Trisakti University|Dharmais National Cancer Center Hospital||October 1 2017||--|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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