Endoxifen-d5 (Z-isomeren)

Endoxifen-d5 (Z-isomer) is the deuterium labeled 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].

1584173-54-5

12352005

Cytochrome P450; Drug Metabolite; Estrogen Receptor/ERR; Isotope-Labeled Compounds; Parasite

Anti-infection; Metabolic Enzyme/Protease; Others; Vitamin D Related/Nuclear Receptor

Cancer

[2H]C([2H])([2H])C([2H])([2H])/C(C1=CC=CC=C1)=C(C2=CC=C(C=C2)O)/C3=CC=C(C=C3)OCCNC

C25H22D5NO2

378.52

[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.

Room temperature

http://file.medchemexpress.com/batch_PDF/HY-18719S/

Isotope-Labeled Compounds

No Development Reported