Endoxifen HCl

Name: Endoxifen HCl
Brand: Selleck Chemicals
SKU: S7839
Rating: 5 (3 reviews)

For research use only.

Catalog No.S7839

3 publications

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

J Mol Cell Biol, 2021, mjab018

PubMed: 33755174 ( click the link to review the publication )

Bone, 2020, 130:115123

PubMed: 31678498 ( click the link to review the publication )

Mol Cell, 2019, 75(6):1103-1116.e9

PubMed: 31420216 ( click the link to review the publication )

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.

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	NH\5eXpHfW6ldHnvckBie3OjeR?=		NH\NVoI1QCCq		MmT6RYdwdmm\|dDDhZ5Rqfmm2eTDheEBGWiCrbjDoeY1idiCPQ1[3PndUQCClZXzsd{Bie3Onc4Pl[EBieyCJUlXCNUBo\W6nIHX4dJJme3Orb36gZZQhOTBpLU[gUUBi\nSncjC0PEBpenNiYomgVnQuWEOUIHHuZYx6e2m\|	NGHKZoczPDhyNUG5PS=>
MCF7 cells	MXrGeY5kfGmxbjDhd5NigQ>?	NH\vVlUyOCC3TR?=	NVLoOXM6PiCq		NH;3ZWhWeHKnZ4XsZZRqd25ib3[gSXJidHCqYTDwdo91\WmwIHzleoVteyCrbjDoeY1idiCPQ1[3JINmdGy\|IHH0JFExKHWPIHHmeIVzKDZiaILzJIJ6KFenc4Tldo4h[myxdDDt[ZRpd2R?	NHr4OHkzPDN\|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]

Protocol

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)

References

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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 Download Endoxifen HCl SDF

Molecular Weight	409.95
Formula	C₂₅H₂₈ClNO₂
CAS No.	1032008-74-4
Storage	3 years-20°C powder 2 years-80°C 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

In vivo Formulation Calculator (Clear solution)

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

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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

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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.

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.

Bio Calculators

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions
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Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
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Molecular Weight Calculator

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2021-05-17)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
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	Recruiting	Drug: Tamoxifen dose adjustment	ER+ Breast Cancer	Nalagenetics Pte Ltd	September 6 2019	Not Applicable
NCT03504631	Unknown status	Other: No intervention	Breast Cancer Female	Trisakti University\|Dharmais National Cancer Center Hospital	October 1 2017	--
NCT01273168	Active not recruiting	Drug: Z-Endoxifen	Hormone Receptor-Positive Breast\|Gynecologic\|Desmoid\|Hormone Receptor-Positive Neoplasms	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	March 1 2011	Phase 1

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Endoxifen HCl