FLTX1 是荧光他莫昔芬衍生物，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。它对子宫的雌激素无激动作用。它在乳腺癌细胞中表现出 Tamoxifen 有效的抗雌激素特性。

FLTX1, 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.

Competition studies showed that FLTX1 binding was totally displaced by unlabeled tamoxifen and partially by estradiol, indicating the existence of non-ER-related triphenylethylene-binding sites.?Ligand binding assays showed that FLTX1 exhibits similar affinity for ER than tamoxifen.?FLTX1 exhibited antiestrogenic activity comparable to tamoxifen in MCF7 and T47D cells transfected with 3xERE-luciferase reporter.?FLTX1 lacked the strong agonistic effect of tamoxifen on ERα-dependent transcriptional activity[1].

In vivo assays in mice revealed that unlike tamoxifen, FLTX1 was devoid of estrogenic uterotrophic effects, lacked of hyperplasic and hypertrophic effects, and failed to alter basal proliferating cell nuclear antigen immunoreactivity.?In the rat uterine model of estrogenicity/antiestrogenicity, FLTX1 displayed antagonistic activity comparable to tamoxifen at lower doses, and only estrogenic uterotrophy at the highest dose[2].

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C31H28N4O4

520.589

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Powder: -20°C for 3 years
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