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Endoxifen hydrochloride

CAS No. : 1197194-41-4

MCE 站：Endoxifen hydrochloride

产品活性：Endoxifen hydrochloride 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。Endoxifen hydrochloride 有用于乳腺癌研究的潜力。

研究领域：Others  |  Metabolic Enzyme/Protease  |  Anti-infection

作用靶点：Estrogen Receptor/ERR  |  Drug Metabolite  |  Parasite  |  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：Bioactive Compound Library Plus  |  Anti-Infection Compound Library  |  Metabolism/Protease Compound Library  |  Anti-Cancer Compound Library  |  Orally Active Compound Library  |  Anti-Breast Cancer Compound Library  |  Chloroquine  |  Tamoxifen  |  Fulvestrant  |  Estradiol  |  Hydroxychloroquine sulfate  |  Clozapine N-oxide  |  4-Hydroxytamoxifen  |  Oseltamivir acid  |  Ivermectin  |  Kaempferol  |  Metronidazole  |  Dihydroartemisinin  |  Niclosamide  |  G15  |  G-1  |  Suramin sodium salt  |  Artesunate  |  Cholesterol  |  Letrozole  |  Urolithin A  |  Artemisinin  |  Bazedoxifene acetate  |  Quinidine  |  PHTPP  |  Halofuginone  |  Miransertib  |  Raloxifene hydrochloride  |  Mefloquine hydrochloride

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