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  3. FLTX1

FLTX1 

Cat. No.: HY-119437
Handling Instructions

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.

For research use only. We do not sell to patients.

FLTX1 Chemical Structure

FLTX1 Chemical Structure

CAS No. : 1481401-71-1

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5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
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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].

IC50 & Target

ERα

87.5 nM (IC50)

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].

MCE 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.
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

520.58

Formula

C₃₁H₂₈N₄O₄

CAS No.

1481401-71-1

SMILES

O=[N+](C1=CC=C(N(CCOC2=CC=C(/C(C3=CC=CC=C3)=C(C4=CC=CC=C4)/CC)C=C2)C)C5=NON=C51)[O-].[(Z)]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

FLTX1FLTX 1FLTX-1Estrogen Receptor/ERRfluorescentTamoxifenestrogenreceptorERpermeabilizednon-permeabilizedantiestrogenicbreastcanceruterusInhibitorinhibitorinhibit

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FLTX1
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