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FLTX1

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FLTX1  纯度: 99.71%

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

FLTX1 Chemical Structure

CAS No. : 1481401-71-1

规格 价格 是否有货 数量
5 mg ￥4500 In-stock
10 mg ￥7500 In-stock
50 mg   询价  
100 mg   询价  

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FLTX1 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library
  • Anti-Breast Cancer Compound Library

生物活性

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].

IC50 & Target

ERα

87.5 nM (IC50)

体外研究
(In Vitro)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell 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.

体内研究
(In Vivo)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

520.58

Formula

C31H28N4O4
CAS 号

1481401-71-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (48.02 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 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

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [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.

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