FLTX1
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MedKoo CAT#: 555964

CAS#: 1481401-71-1

Description: FLTX1 is a fluorescent Tamoxifen derivative that can specifically label intracellular Tamoxifen-binding sites (estrogen receptors). FLTX1 allows the labeling of estrogen receptors in immunocytochemistry and immunohistochemistry studies, both under permeabilized and non-permeabilized conditions. FLTX1 showed the pharmacological activity of the tamoxifen moiety and efficient fluorescence properties, which could be used synergistically to improve the effect of the drug.


Chemical Structure

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FLTX1
CAS# 1481401-71-1

Theoretical Analysis

MedKoo Cat#: 555964
Name: FLTX1
CAS#: 1481401-71-1
Chemical Formula: C31H28N4O4
Exact Mass: 520.21
Molecular Weight: 520.589
Elemental Analysis: C, 71.52; H, 5.42; N, 10.76; O, 12.29

Price and Availability

Size Price Availability Quantity
10mg USD 150 Ready to ship
25mg USD 250 Ready to ship
50mg USD 450 Ready to ship
100mg USD 750 Ready to ship
200mg USD 1250 Ready to ship
500mg USD 2650 Ready to ship
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Synonym: FLTX1; FLTX-1; FLTX 1;

IUPAC/Chemical Name: N-[2-[4-[(1Z)-1,2-Diphenyl-1-buten-1-yl]phenoxy]ethyl]-N-methyl-7-nitro-2,1,3-benzoxadiazol-4-amine

InChi Key: UKSXWLGSDIHAEK-WCTVFOPTSA-N

InChi Code: InChI=1S/C31H28N4O4/c1-3-26(22-10-6-4-7-11-22)29(23-12-8-5-9-13-23)24-14-16-25(17-15-24)38-21-20-34(2)27-18-19-28(35(36)37)31-30(27)32-39-33-31/h4-19H,3,20-21H2,1-2H3/b29-26-

SMILES Code: 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-]

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info: 1: Lahoz F, Scholz LE, Boto A, Díaz M. FRET mechanism between a fluorescent breast-cancer drug and photodynamic therapy sensitizers. Spectrochim Acta A Mol Biomol Spectrosc. 2020 Oct 5;239:118498. doi: 10.1016/j.saa.2020.118498. Epub 2020 May 19. PMID: 32470814. 2: Morales A, Marín R, Marrero-Alonso J, Boto A, Díaz M. Colocalization of Estrogen Receptors with the Fluorescent Tamoxifen Derivative, FLTX1, Analyzed by Confocal Microscopy. Methods Mol Biol. 2016;1366:163-173. doi: 10.1007/978-1-4939-3127-9_13. PMID: 26585134. 3: Marrero-Alonso J, Morales A, García Marrero B, Boto A, Marín R, Cury D, Gómez T, Fernández-Pérez L, Lahoz F, Díaz M. Unique SERM-like properties of the novel fluorescent tamoxifen derivative FLTX1. Eur J Pharm Biopharm. 2013 Nov;85(3 Pt B):898-910. doi: 10.1016/j.ejpb.2013.04.024. Epub 2013 May 31. PMID: 23727370.

Biological target: FLTX1 is a fluorescent Tamoxifen derivative that can specifically label intracellular Tamoxifen-binding sites (estrogen receptors) under permeabilized and non-permeabilized conditions.
In vitro activity: 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. Reference: Eur J Pharm Biopharm. 2013 Nov;85(3 Pt B):898-910. https://pubmed.ncbi.nlm.nih.gov/23727370/
In vivo activity: 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. Reference: Eur J Pharm Biopharm. 2013 Nov;85(3 Pt B):898-910. https://pubmed.ncbi.nlm.nih.gov/23727370/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 25.0 48.02

Preparing Stock Solutions

The following data is based on the product molecular weight 520.59 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: Marrero-Alonso J, Morales A, García Marrero B, Boto A, Marín R, Cury D, Gómez T, Fernández-Pérez L, Lahoz F, Díaz M. Unique SERM-like properties of the novel fluorescent tamoxifen derivative FLTX1. Eur J Pharm Biopharm. 2013 Nov;85(3 Pt B):898-910. doi: 10.1016/j.ejpb.2013.04.024. Epub 2013 May 31. PMID: 23727370.
In vitro protocol: Marrero-Alonso J, Morales A, García Marrero B, Boto A, Marín R, Cury D, Gómez T, Fernández-Pérez L, Lahoz F, Díaz M. Unique SERM-like properties of the novel fluorescent tamoxifen derivative FLTX1. Eur J Pharm Biopharm. 2013 Nov;85(3 Pt B):898-910. doi: 10.1016/j.ejpb.2013.04.024. Epub 2013 May 31. PMID: 23727370.
In vivo protocol: Marrero-Alonso J, Morales A, García Marrero B, Boto A, Marín R, Cury D, Gómez T, Fernández-Pérez L, Lahoz F, Díaz M. Unique SERM-like properties of the novel fluorescent tamoxifen derivative FLTX1. Eur J Pharm Biopharm. 2013 Nov;85(3 Pt B):898-910. doi: 10.1016/j.ejpb.2013.04.024. Epub 2013 May 31. PMID: 23727370.

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