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。

FLTX1 is a fluorescent Tamoxifen derivative that can specifically label intracellular Tamoxifen-binding sites (estrogen receptors) under permeabilized and non-permeabilized conditions. FLTX1 exhibits the potent antiestrogenic properties of Tamoxifen in breast cancer cells. FLTX1 is devoid of the estrogenic agonistic effect on the uterus.

Solid

ERα 87.5 nM (IC50)

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 [H] 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. has not independently confirmed the accuracy of these methods.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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Powder -20°C 3 years；4°C 2 years

[1]. Marrero-Alonso J, et, al. Unique SERM-like properties of the novel fluorescent tamoxifen derivative FLTX1. Eur J Pharm Biopharm. 2013 Nov;85(3 Pt B):898-910.
[2]. Morales A, et, al. Colocalization of Estrogen Receptors with the Fluorescent Tamoxifen Derivative, FLTX1, Analyzed by Confocal Microscopy. Methods Mol Biol. 2016;1366:163-173.

In Vitro: DMSO : 25 mg/mL (48.02 mM; Need ultrasonic)配制储备液