Endoxifen (Z-isomer)Endoxifen (Z-isomer)
MedChemExpress (MCE)
HY-18719
112093-28-4
99.20%
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Room temperature in continental US
may vary elsewhere.
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.
Z-Endoxifen (Z-isomer) (0.1-5 μM, 7 days) exhibits potent antiproliferative activity against MCF7AC1 and MCF7LR cell lines[4].
Z-Endoxifen (Z-isomer) (5 mg/kg/day, s.c., gradual drug release every 30 days, pellets replaced every 90 days) effectively prevents breast cancer in the C3(1)-TAg mouse model[3]. Z-Endoxifen (50 mg/kg, p.o., 5 times a week for 4 weeks) shows better antitumor efficacy in the MCF7LR resistant mouse model[4]. Z-Endoxifen (75 mg/kg, p.o., once daily for 4 weeks) shows strong antitumor activity in the MCF7AC1 mouse breast cancer model[4].
| | | |
| | | | | |
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]