For research use only.
CAS No. 1032008-74-4
Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.
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|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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|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
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|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04315792||Recruiting||Drug: Endoxifen|Drug: Placebo oral tablet||Bipolar I Disorder||Jina Pharmaceuticals Inc.|Novum Pharmaceutical Research Services|Lambda Therapeutic Research Ltd.|Intas Pharmaceuticals Ltd.||March 23 2020||Phase 3|
|NCT04312347||Recruiting||Drug: Tamoxifen dose adjustment||ER+ Breast Cancer||Nalagenetics Pte Ltd||September 6 2019||Not Applicable|
|NCT03504631||Unknown status||Other: No intervention||Breast Cancer Female||Trisakti University|Dharmais National Cancer Center Hospital||October 1 2017||--|
|NCT01273168||Active not recruiting||Drug: Z-Endoxifen||Hormone Receptor-Positive Breast|Gynecologic|Desmoid|Hormone Receptor-Positive Neoplasms||National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)||March 1 2011||Phase 1|
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