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FLTX1 Sale

目录号 : GC62484

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 Chemical Structure

Cas No.:1481401-71-1

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,662.00
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1mg
¥553.00
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5mg
¥1,452.00
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10mg
¥2,172.00
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25mg
¥3,522.00
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50mg
¥4,838.00
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Sample solution is provided at 25 µL, 10mM.

Description

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[1][2].

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[1].FLTX1 (50 μM; 2 h) exhibits a dose-dependent competition with Tamoxifen (Tx) in MCF7 cells[1].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[1].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[1].

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[1].

[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.

化学性质

Cas No. 1481401-71-1 SDF
分子式 C31H28N4O4 分子量 520.58
溶解度 DMSO : 25 mg/mL (48.02 mM; Need ultrasonic) 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 1.9209 mL 9.6047 mL 19.2093 mL
5 mM 0.3842 mL 1.9209 mL 3.8419 mL
10 mM 0.1921 mL 0.9605 mL 1.9209 mL
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