Endoxifen hydrochloride

Research use only, not for human use.

A metabolite of tamoxifen, orally active non-steroidal selective estrogen receptor modulator (SERM) for the treatment of estrogen receptor-positive breast cancer.

A metabolite of tamoxifen, orally active non-steroidal selective estrogen receptor modulator (SERM) for the treatment of estrogen receptor-positive breast cancer.Breast Cancer Phase 1 Clinical.

Endoxifen, a hydroxylated Tamoxifen metabolite, is approximately 100-fold more potent as an antagonist of the ER than tamoxifen. It also suggests that endoxifen but not 4-hydroxytamoxifen results in ER-alpha degradation in addition to its effects on the ER at the level of transcription. Endoxifen, is a potent antiestrogen that targets estrogen receptor α for degradation in breast cancer cells. Additionally, it is showed that Endoxifen blocks ERA transcriptional activity and inhibits estrogen-induced breast cancer cell proliferation even in the presence of tamoxifen, N-desmethyl-tamoxifen, and 4-hydroxytamoxifen. Endoxifen is strongly growth inhibitory at 10 μM for all the breast cancer cell lines except for moderate inhibition for MDAMB-468.Cytotoxic effects are quite significant at 10 μM concentration for MCF7, HS 578T, and BT-549 cells. At lower Endoxifen concentrations (0.01-1 μM), the inhibitory effects are not as significant as 10 μM, whereas 100 μM Endoxifen concentration found to be lethal for all tested cells.

Orally administered Endoxifen is rapidly absorbed and systemically available when tested in female rats. The Endoxifen-treated rats show 787% higher exposure (AUC0–∞) and 1,500% higher concentration (Cmax) levels of Endoxifen when compared with Tamoxifen. Oral Endoxifen administration once a day for 28 consecutive days at dosages 2, 4, and 8 mg/kg proves safe and results in progressive inhibition of the growth of the human mammary tumor xenografts in female mice.

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Endocrinology/Hormones

Estrogen Receptor/ERR

Estrogen Receptor/ERR

Cancer

Breast Cancer

1197194-41-4

409.9483

C25H28ClNO2

>98% (HPLC)

DMSO: ≥ 35 mg/mL

CCC(=C(C1=CC=C(C=C1)O)C2=CC=C(C=C2)OCCNC)C3=CC=CC=C3.Cl

Phenol, 4-[1-[4-[2-(methylamino)ethoxy]phenyl]-2-phenyl-1-buten-1-yl]-, hydrochloride (1:1)

(-20℃)

With Ice Pack

≥ 2 years