Endoxifen (Z-isomer)

Endoxifen Z-isomer is an oral active Tamoxifen (HY-13757A) metabolite, inducing an anti-estrogenic effect in breast cancer cells expressing ERα. Endoxifen Z-isomer inhibits hERG. This effect is concentration-dependent, with an IC50 value of 1.6 μM[1][2][3][4].

Product Specifications

CAS Number

[112093-28-4]

UNSPSC

12352005

Hazard Statement

H315-H319-H335

Target

Estrogen Receptor/ERR; Potassium Channel

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel; Vitamin D Related/Nuclear Receptor

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Endoxifen-Z-isomer.html

Purity

99.19

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

OC1=CC=C(/C(C2=CC=C(OCCNC)C=C2)=C(C3=CC=CC=C3)\CC)C=C1

Molecular Formula

C25H27NO2

Molecular Weight

373.49

Precautions

P261-P264-P271-P280-P302+P352-P304+P340-P305+P351+P338-P362-P403+P233-P405-P501

References & Citations

[1]Chae YJ, et al. Endoxifen, the active metabolite of tamoxifen, inhibits cloned hERG potassium channels. Eur J Pharmacol. 2015 Apr 5;752:1-7.|[2]Wu X, et al. Estrogen receptor-beta sensitizes breast cancer cells to the anti-estrogenic actions of endoxifen. Breast Cancer Res. 2011 Mar 10;13 (2) :R27.|[3]Lee O, et al. Z-Endoxifen prevents aggressive mammary cancers in mice by inhibiting cell proliferation and creating a tumor suppressive microenvironment. Biomed Pharmacother. 2023 Jun;162:114607.|[4]Jayaraman S, et al. Antitumor activity of Z-endoxifen in aromatase inhibitor-sensitive and aromatase inhibitor-resistant estrogen receptor-positive breast cancer. Breast Cancer Res. 2020 May 19;22 (1) :51.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Phase 3

Citation 01

North Dakota State University of Agriculture and Applied Science. 2018 Feb.|J Chromatogr B Analyt Technol Biomed Life Sci. 2024 Apr 15:1237:124100.|Sci Rep. 2022 Jan 31;12 (1) :1643.