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)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01273168||Active not recruiting||Hormone Receptor-Positive Breast|Gynecologic|Desmoid|Hormone Receptor-Positive Neoplasms||National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)||January 7 2011||Phase 1|
|NCT02311933||Active not recruiting||Estrogen Receptor Positive|HER2/Neu Negative|Recurrent Breast Carcinoma|Stage III Breast Cancer AJCC v7|Stage IIIA Breast Cancer AJCC v7|Stage IIIB Breast Cancer AJCC v7|Stage IIIC Breast Cancer AJCC v7|Stage IV Breast Cancer AJCC v6 and v7||National Cancer Institute (NCI)||March 6 2015||Phase 2|
|NCT01327781||Active not recruiting||Estrogen Receptor Positive|HER2/Neu Positive|Hot Flashes|Recurrent Breast Carcinoma|Stage IIIC Breast Cancer AJCC v7|Stage IV Breast Cancer AJCC v6 and v7||National Cancer Institute (NCI)||March 25 2011||Phase 1|
|NCT03317405||Not yet recruiting||BRCA1 Gene Mutation|BRCA2 Gene Mutation|Ductal Breast Carcinoma In Situ|Lobular Breast Carcinoma In Situ|Prophylactic Mastectomy Patient|Stage 0 Breast Cancer AJCC v6 and v7|Stage I Breast Cancer AJCC v7|Stage IA Breast Cancer AJCC v7|Stage IB Breast Cancer AJCC v7|Stage II Breast Cancer AJCC v6 and v7|Stage IIA Breast Cancer AJCC v6 and v7|Stage IIB Breast Cancer AJCC v6 and v7|Stage III Breast Cancer AJCC v7|Stage IIIA Breast Cancer AJCC v7|Stage IIIB Breast Cancer AJCC v7|Stage IIIC Breast Cancer AJCC v7||National Cancer Institute (NCI)||October 15 2018||Phase 1|
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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