FLTX1

Research use only, not for human use.

FLTX1, a fluorescent Tamoxifen derivative that can specifically label intracellular Tamoxifen-binding sites (estrogen receptors) under permeabilized and non-permeabilized conditions.

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.

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. Cell Proliferation AssayCell Line:MCF7 cells Concentration:0.01, 0.1, 1, 5, 10 μM Incubation Time:6 days Result:Inhibited MCF7 cell proliferation in a dose-dependent manner, being significantly more effective than Tx already at 0.1 μM.

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.

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Endocrinology/Hormones

Estrogen Receptor/ERR

ERα

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1481401-71-1

520.6

C31H28N4O4

>98% (HPLC)

DMSO:10 mM

CCC(=C(C1=CC=CC=C1)C2=CC=C(C=C2)OCCN(C)C3=CC=C(C4=NON=C34)[N+](=O)[O-])C5=CC=CC=C5

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(-20℃)

With Ice Pack

≥ 2 years