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Endoxifen HCl Estrogen/progestogen Receptor antagonist

Name: Endoxifen HCl
Brand: Selleck Chemicals
SKU: S7839
Availability: InStock
Rating: 5 (6 reviews)

Cat.No.S7839

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

Chemical Structure

Molecular Weight: 409.95

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.81%

99.81

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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description
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
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
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	409.95	Formula	C₂₅H₂₈ClNO₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1032008-74-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CCC(=C(C1=CC=C(C=C1)O)C2=CC=C(C=C2)OCCNC)C3=CC=CC=C3.Cl

Solubility

In vitro
Batch:

DMSO : 81 mg/mL (197.58 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 81 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5% DMSO 1 20% PEG 300 2 5%Tween80 3 70% water Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.500mg/ml (6.10mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 200 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; then continue adding Adjust the volume to 1 mL with 700 μL ddH2O. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.300mg/ml (0.73mM)	Taking the 1 mL working solution as an example, add 50 μL of 6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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+ %

Calculation results:

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.

Mechanism of Action

Targets/IC₅₀/Ki	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]
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]
References	[1] https://pubmed.ncbi.nlm.nih.gov/15685451/ [2] https://pubmed.ncbi.nlm.nih.gov/19244106/ [3] https://pubmed.ncbi.nlm.nih.gov/20052538/ [4] https://pubmed.ncbi.nlm.nih.gov/20227879/ [5] https://pubmed.ncbi.nlm.nih.gov/25680947/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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	Unknown status	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

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