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Endoxifen

CAS No. : 110025-28-0

MCE 站：Endoxifen

产品活性：Endoxifen 是tamoxifen 的关键活性代谢物，与雌激素受体 (estrogen receptor) 有较高的亲和力和特异性，同时也能抑制芳香酶的活性。

研究领域：Others

作用靶点：Estrogen Receptor/ERR  |  Aromatase

In Vitro: 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.

In Vivo: Orally administered Endoxifen is rapidly absorbed and systemically available when tested in female rats. The Endoxifen-treated rats show 787% higher exposure (AUC_0–∞) and 1,500% higher concentration (C_max) 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.

相关产品：Tamoxifen  |  Fulvestrant  |  Estradiol  |  4-Hydroxytamoxifen  |  Kaempferol  |  Letrozole  |  G-1  |  AZD9496  |  Elacestrant dihydrochloride  |  PHTPP  |  Cholesterol  |  Raloxifene hydrochloride  |  Bazedoxifene acetate  |  G15  |  DPN  |  27-Hydroxycholesterol  |  Exemestane  |  XCT790  |  Diethylstilbestrol  |  Estrone  |  Anastrozole  |  Clomiphene citrate  |  Fadrozole hydrochloride  |  Saikosaponin D  |  Brilanestrant  |  Chrysin  |  Endoxifen hydrochloride

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