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FLTX1

Catalog No. T8984 CAS 1481401-71-1

FLTX1 is a fluorescent derivative of Tamoxifen, designed to efficiently target and label intracellular Tamoxifen-binding sites (estrogen receptors) both under permeabilized and non-permeabilized conditions. Additionally, FLTX1 demonstrates strong antiestrogenic activity in breast cancer cells, resembling the potent antiestrogenic properties of Tamoxifen. Notably, FLTX1 does not exhibit any estrogenic agonistic effect on the uterus.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

FLTX1, CAS 1481401-71-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 98.00
5 mg	In stock	$ 263.00
10 mg	In stock	$ 413.00
25 mg	In stock	$ 692.00
50 mg	In stock	$ 985.00
100 mg	In stock	$ 1,330.00
500 mg	In stock	$ 2,660.00
1 mL * 10 mM (in DMSO)	In stock	$ 288.00

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Purity: 98.46%

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Description	FLTX1 is a fluorescent derivative of Tamoxifen, designed to efficiently target and label intracellular Tamoxifen-binding sites (estrogen receptors) both under permeabilized and non-permeabilized conditions. Additionally, FLTX1 demonstrates strong antiestrogenic activity in breast cancer cells, resembling the potent antiestrogenic properties of Tamoxifen. Notably, FLTX1 does not exhibit any estrogenic agonistic effect on the uterus.
Targets&IC50	ERα:87.5 nM
In vitro	Competition studies showed that FLTX1 binding was totally displaced by unlabeled tamoxifen and partially by estradiol, indicating the existence of non-ER-related triphenylethylene-binding sites.?Ligand binding assays showed that FLTX1 exhibits similar affinity for ER than tamoxifen.?FLTX1 exhibited antiestrogenic activity comparable to tamoxifen in MCF7 and T47D cells transfected with 3xERE-luciferase reporter.?FLTX1 lacked the strong agonistic effect of tamoxifen on ERα-dependent transcriptional activity[1].
In vivo	In vivo assays in mice revealed that unlike tamoxifen, FLTX1 was devoid of estrogenic uterotrophic effects, lacked of hyperplasic and hypertrophic effects, and failed to alter basal proliferating cell nuclear antigen immunoreactivity.?In the rat uterine model of estrogenicity/antiestrogenicity, FLTX1 displayed antagonistic activity comparable to tamoxifen at lower doses, and only estrogenic uterotrophy at the highest dose[2].

Molecular Weight	520.58
Formula	C31H28N4O4
CAS No.	1481401-71-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 5.21 mg/mL (10 mM), Sonication is recommended.

References and Literature

1. https://pubmed.ncbi.nlm.nih.gov/23727370/ 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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Anti-Ovarian Cancer Compound Library Nuclear Receptor Compound Library Anti-Breast Cancer Compound Library Endocrinology-Hormone Compound Library Bioactive Compounds Library Max Bioactive Compound Library NO PAINS Compound Library Anti-Cancer Compound Library

Related Products

Related compounds with same targets

5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone Genistin XCT790 Endoxifen (E-isomer) Estrogen receptor modulator 7 Estrone G-1 Raloxifene hydrochloride

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Keywords

FLTX1 1481401-71-1 Endocrinology/Hormones Estrogen Receptor/ERR Estrogen/progestogen Receptor cancer Inhibitor fluorescent Tamoxifen antiestrogenic inhibit non-permeabilized receptor breast FLTX 1 estrogen permeabilized FLTX-1 uterus inhibitor

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