Home Endocrinology & Hormones Estrogen/progestogen Receptor antagonist Endoxifen HCl

Endoxifen HCl

Catalog No.S7839

For research use only.

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

Endoxifen HCl Chemical Structure

CAS No. 1032008-74-4

Selleck's Endoxifen HCl has been cited by 3 Publications

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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  NXTjbZlMTnWwY4Tpc44h[XO|YYm= MYW0PEBp MYDB[49vcXO2IHHjeIl3cXS7IHH0JGVTKGmwIHj1cYFvKE2FRke6W3M5KGOnbHzzJIF{e2W|c3XkJIF{KEeURVKxJIdmdmViZYjwdoV{e2mxbjDheEAyOCdvNjDNJIFnfGW{IES4JIhzeyCkeTDSWE1RS1JiYX7hcJl{cXN? MWeyOFgxPTF7OR?=
MCF7 cells NXnMPJppTnWwY4Tpc44h[XO|YYm= MYixNEB2VQ>? MVu2JIg> MXLVdJJm\3WuYYTpc44hd2ZiRWLhcJBp[SCycn;0[YlvKGyndnXsd{BqdiCqdX3hckBOS0Z5IHPlcIx{KGG2IEGwJJVOKGGodHXyJFYhcHK|IHL5JHdme3Sncn6gZoxwfCCvZYToc4Q> MnrLNlQ{OzJ4M{C=
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 (from reference)

Cell Research:[2]
  • 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]
  • 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
Formula

C25H28ClNO2
CAS No. 1032008-74-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCC(=C(C1=CC=C(C=C1)O)C2=CC=C(C=C2)OCCNC)C3=CC=CC=C3.Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05133674 Not yet recruiting Drug: Tamoxifen 20 mg Breast Cancer|Breast Carcinoma|Breast Tumors|Cancer of Breast|Malignant Neoplasm of Breast Karolinska University Hospital January 10 2022 Phase 2
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 --

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

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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