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Endoxifen HCl

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

Catalog No.S7839

For research use only.

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

CAS No. 1032008-74-4

Selleck's Endoxifen HCl has been cited by 5 Publications

Purity & Quality Control

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Estrogen/progestogen Receptor Signaling Pathways

Estrogen/progestogen Receptor Signaling Pathway Map

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	NED3XXBHfW6ldHnvckBie3OjeR?=		NIG4N4s1QCCq		MkLERYdwdmm\|dDDhZ5Rqfmm2eTDheEBGWiCrbjDoeY1idiCPQ1[3PndUQCClZXzsd{Bie3Onc4Pl[EBieyCJUlXCNUBo\W6nIHX4dJJme3Orb36gZZQhOTBpLU[gUUBi\nSncjC0PEBpenNiYomgVnQuWEOUIHHuZYx6e2m\|	M{TadFI1QDB3MUm5
MCF7 cells	M2fsfGZ2dmO2aX;uJIF{e2G7	NIXwOJAyOCC3TR?=	MX22JIg>		NGjXdZNWeHKnZ4XsZZRqd25ib3[gSXJidHCqYTDwdo91\WmwIHzleoVteyCrbjDoeY1idiCPQ1[3JINmdGy\|IHH0JFExKHWPIHHmeIVzKDZiaILzJIJ6KFenc4Tldo4h[myxdDDt[ZRpd2R?	MmTONlQ{OzJ4M{C=

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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.

Animal Research:^[3]

Animal Models: Mice bearing MCF-7 human mammary tumor xenografts
Dosages: 8 mg/kg
Administration: p.o.

References

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Solubility (25°C)

In vitro

Chemical Information

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

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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

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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.

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
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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

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