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FLTX1

CAS No. : 1481401-71-1

MCE 站：FLTX1

产品活性：FLTX1 是一种荧光他莫昔芬 (Tamoxifen) 衍生物，可以在透化和非透化条件下特异性标记细胞内 Tamoxifen 结合位点 (雌激素受体)。FLTX1 在乳腺癌细胞中表现出 Tamoxifen 有效的抗雌激素特性。FLTX1 缺乏对子宫的雌激素激动作用。

研究领域：Others

作用靶点：Estrogen Receptor/ERR

In Vitro: FLTX1 (0.01-10 μM; 6 d) reduces MCF7 cell proliferation in a dose-dependent manner. FLTX1 (pretreated 24 h) counteracts the increase in cell growth induced by E₂ down to the vehicle level.
FLTX1 (50 μM; 2 h) exhibits a dose-dependent competition with Tamoxifen (Tx) in MCF7 cells.
FLTX1 (0.1 nM-100 μM; 18 h) competitively displaces the [³H] E₂ binding to rat uterine estrogen receptors (ER) rat uterus cytosol, with an IC₅₀ of 87.5 nM.
FLTX1 (0.1 nM-10 μM; pretreated 8 h) reduces the estradiol-induced luciferase expression activity in a dose-dependent manner. FLTX1 (15-16 h) is devoid of the potent estrogenic agonist activity in both transiently transfected MCF7 cells and stably transfected T47D-KBluc cells.

In Vivo: FLTX1 (0.01-1 mg/kg/d; s.c. for 3 d) is lacked of the estrogenic uterotrophic (and also cervical and vaginal), hyperplasic and hypertrophic effects, and failed to alter basal proliferating cell nuclear antigen immunoreactivity in mice and rats.

相关产品：Bioactive Compound Library Plus  |  Anti-Cancer Compound Library  |  Anti-Breast Cancer Compound Library  |  Tamoxifen  |  Fulvestrant  |  Estradiol  |  4-Hydroxytamoxifen  |  Kaempferol  |  G15  |  G-1  |  Cholesterol  |  Bazedoxifene acetate  |  PHTPP  |  Raloxifene hydrochloride  |  DPN  |  Estrone  |  Chrysin  |  (-)-(S)-Equol  |  27-Hydroxycholesterol  |  Liquiritigenin  |  Propyl pyrazole triol  |  Toremifene citrate  |  Genistin  |  Diethylstilbestrol  |  Saikosaponin D  |  Lasofoxifene Tartrate  |  (20S)-Protopanaxatriol  |  Estriol  |  Prinaberel  |  Clomiphene citrate  |  Kaempferide

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