FLTX1  ≥98%

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沸点:679.5±65.0 °C(Predicted)
密度:1.258±0.06 g/cm3(Predicted)
包装规格:1mg 5mg 10mg 25mg 50mg 100mg 200mg in glass bottle
产品简介: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。
溶解性:DMSO : 25 mg/mL (48.02 mM; Need ultrasonic)
储备液保存:-80°C, 6 months; -20°C, 1 month。
靶点:ERα:87.5 nM (IC50)
体外研究: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.
体内研究: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.
保存条件:-20°C 密封干燥
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