Endoxifen HCl

Catalog No.S7839

Endoxifen HCl Chemical Structure

Molecular Weight(MW): 409.95

Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.

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Biological Activity

Description Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.
Targets
Estrogen receptor [1]
In vitro

Endoxifen shows anti-estrogenic effects, and decreases the E2-induced PR expression in MCF-7 cells. [1] Endoxifen also blocks ER-alpha transcriptional activity and inhibits estrogen-induced breast cancer cell proliferation. [2] In MCF7, HS 578T, and BT-549 cells, Endoxifen significantly inhibits cell proliferation. [3] Endoxifen also exhibits four-fold higher inhibition on PKC activity compared to tamoxifen. [4] Endoxifen inhibits the hERG current by preferentially interacting with the activated states of cloned hERG potassium channels with IC50 of 1.6 μM. [5]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF7:WS8 cells  MnThSpVv[3Srb36gZZN{[Xl? NET5PVc1QCCq M4\PdGFod26rc4SgZYN1cX[rdImgZZQhTVJiaX6gbJVu[W5iTVPGO|pYWzhiY3XscJMh[XO|ZYPz[YQh[XNiR2LFRlEh\2WwZTDlfJBz\XO|aX;uJIF1KDFyJz22JG0h[W[2ZYKgOFghcHK|IHL5JHJVNVCFUjDhcoFtgXOrcx?= M4H6U|I1QDB3MUm5
MCF7 cells M1jndWZ2dmO2aX;uJIF{e2G7 NIj0RVUyOCC3TR?= MVy2JIg> M4LvZ3VxemWpdXzheIlwdiCxZjDFVoFteGijIIDyc5RmcW5ibHX2[Yx{KGmwIHj1cYFvKE2FRkegZ4VtdHNiYYSgNVAhfU1iYX\0[ZIhPiCqcoOgZpkhX2W|dHXyckBjdG:2IH3leIhw\A>? NYTLbos5OjR|M{K2N|A>

... Click to View More Cell Line Experimental Data
In vivo In vivo, Endoxifen (8 mg/kg, ) inhibits growth of MCF-7 human mammary tumor xenografts in mice, showing more potency than Tamoxifen. [3]

Protocol

Cell Research:[2]
+ Expand
  • Cell lines: MCF7 and Ishikawa cells
  • Concentrations: 1000 nM
  • Incubation Time: 8 days
  • Method: MCF7 and Ishikawa cells are grown in 10% triple charcoal-stripped serum-containing medium for 3 d. The cells are then plated at a density of 2,000 cells per well in 96-well tissue culture plates and treated as indicated every 48 h. Cell proliferation assays are conducted 8 days after the first treatment using a CellTiter-Glo Luminescent Cell Viability kit according to the manufacturer's protocol.
    (Only for Reference)
Animal Research:[3]
+ Expand
  • Animal Models: Mice bearing MCF-7 human mammary tumor xenografts
  • Formulation: Water
  • Dosages: 8 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 74 mg/mL (180.5 mM)
Ethanol 74 mg/mL (180.5 mM)
Water Insoluble

* 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.

Chemical Information

Molecular Weight 409.95
Formula

C25H28ClNO2
CAS No. 1032008-74-4
Storage powder
in solvent
Synonyms N/A

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID