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FLTX1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
FLTX1图片
CAS NO:1481401-71-1

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。
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 breastcancercells. 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 E2down 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] E2binding to rat uterine estrogen receptors (ER) rat uterus cytosol, with an IC50of 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].

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].

分子量

520.58

性状

Solid

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°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 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 mg5 mg10 mg
1 mM1.9209 mL9.6047 mL19.2093 mL
5 mM0.3842 mL1.9209 mL3.8419 mL
10 mM0.1921 mL0.9605 mL1.9209 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

 
 
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