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FLTX1

SKU: orb1218779

Description

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.

Images & Validation

Key Properties

CAS Number1481401-71-1
MW520.6
Purity>98% (HPLC)
FormulaC31H28N4O4
SMILESCCC(=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
TargetEstrogen Receptor/ERR
SolubilityDMSO:10 mM

Bioactivity

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.
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. 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 Assay 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.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

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    1481401-71-1

    520.58

    C31H28N4O4

    5 mg, 10 mg, 1 mg, 25 mg, 50 mg, 100 mg, 200 mg, 1 ml x 10 mM (in DMSO)
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FLTX1 (orb1218779)

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Available Sizes

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5 mg
¥ 4,810.00
10 mg
¥ 7,280.00
25 mg
¥ 11,830.00
50 mg
¥ 16,770.00
100 mg
¥ 22,490.00
500 mg
¥ 44,460.00