Endoxifen HCl

For research use only.

Catalog No.S7839

3 publications

Endoxifen HCl Chemical Structure

CAS No. 1032008-74-4

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

Selleck's Endoxifen HCl has been cited by 3 publications

Purity & Quality Control

Choose Selective Estrogen/progestogen Receptor Inhibitors

Biological Activity

Description Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.
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  MYXGeY5kfGmxbjDhd5NigQ>? Mnm5OFghcA>? Moj0RYdwdmm|dDDhZ5Rqfmm2eTDheEBGWiCrbjDoeY1idiCPQ1[3PndUQCClZXzsd{Bie3Onc4Pl[EBieyCJUlXCNUBo\W6nIHX4dJJme3Orb36gZZQhOTBpLU[gUUBi\nSncjC0PEBpenNiYomgVnQuWEOUIHHuZYx6e2m| NFnBeWIzPDhyNUG5PS=>
MCF7 cells MUDGeY5kfGmxbjDhd5NigQ>? NHq2fpYyOCC3TR?= NFWwNYQ3KGh? MV;VdJJm\3WuYYTpc44hd2ZiRWLhcJBp[SCycn;0[YlvKGyndnXsd{BqdiCqdX3hckBOS0Z5IHPlcIx{KGG2IEGwJJVOKGGodHXyJFYhcHK|IHL5JHdme3Sncn6gZoxwfCCvZYToc4Q> NEjaUoQzPDN|Mk[zNC=>

... 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]


Cell Research:[2]
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  • 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]
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  • Animal Models: Mice bearing MCF-7 human mammary tumor xenografts
  • 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


CAS No. 1032008-74-4
Storage powder
in solvent
Synonyms N/A
Smiles CCC(=C(C1=CC=C(C=C1)O)C2=CC=C(C=C2)OCCNC)C3=CC=CC=C3.Cl

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04961632 Recruiting Drug: Tamoxifen Breast Cancer National Cancer Centre Singapore|National Medical Research Council (NMRC) Singapore December 23 2020 Phase 1
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 Completed Drug: Tamoxifen dose adjustment ER+ Breast Cancer Nalagenetics Pte Ltd September 6 2019 Not Applicable
NCT03582865 Unknown status Drug: Tamoxifen 20 mg Breast Cancer Assiut University September 1 2019 --

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Estrogen/progestogen Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID