Home Endocrinology & Hormones Estrogen/progestogen Receptor antagonist Endoxifen HCl For research use only.

Endoxifen HCl

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

Endoxifen HCl Chemical Structure

Endoxifen HCl Chemical Structure

CAS: 1032008-74-4

Selleck's Endoxifen HCl has been cited by 5 publications

Purity & Quality Control

Batch: Purity: 99.81%
99.81

Endoxifen HCl Related Products

Signaling Pathway

Estrogen/progestogen Receptor Signaling Pathways

Estrogen/progestogen Receptor Signaling Pathway

Choose Selective Estrogen/progestogen Receptor Inhibitors

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF7:WS8 cells  Function assay 48 h Agonist activity at ER in human MCF7:WS8 cells assessed as GREB1 gene expression at 10'-6 M after 48 hrs by RT-PCR analysis 24805199
MCF7 cells Function assay 10 uM 6 h Upregulation of ERalpha protein levels in human MCF7 cells at 10 uM after 6 hrs by Western blot method 24332630
Click to View More Cell Line Experimental Data

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
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 Research 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.
In Vivo
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]
Animal Research Animal Models Mice bearing MCF-7 human mammary tumor xenografts
Dosages 8 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05607004 Recruiting
Breast Neoplasms|Invasive Breast Cancer|Estrogen-receptor-positive Breast Cancer|HER2-negative Breast Cancer
Atossa Therapeutics Inc.|InClin
 February 14 2023 Phase 2
NCT05133674 Active not recruiting
Breast Cancer|Breast Carcinoma|Breast Tumors|Cancer of Breast|Malignant Neoplasm of Breast
Karolinska University Hospital
 April 4 2022 Phase 2
NCT04961632 Active not recruiting
Breast Cancer
National Cancer Centre Singapore|National Medical Research Council (NMRC) Singapore
 December 23 2020 Phase 1
NCT04315792 Recruiting
Bipolar I Disorder
Jina Pharmaceuticals Inc.|Novum Pharmaceutical Research Services|Lambda Therapeutic Research Ltd.|Intas Pharmaceuticals Ltd.
 March 23 2020 Phase 3
NCT04312347 Completed
ER+ Breast Cancer
Nalagenetics Pte Ltd
 September 6 2019 Not Applicable

Chemical Information & Solubility

Molecular Weight 409.95 Formula

C25H28ClNO2
CAS No. 1032008-74-4 SDF Download Endoxifen HCl SDF
Smiles CCC(=C(C1=CC=C(C=C1)O)C2=CC=C(C=C2)OCCNC)C3=CC=CC=C3.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 81 mg/mL ( (197.58 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 81 mg/mL

Water : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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.

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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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