WARNING: This product is for research use only, not for human or veterinary use.
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.
MedKoo Cat#: 555964
Name: FLTX1
CAS#: 1481401-71-1
Chemical Formula: C31H28N4O4
Exact Mass: 520.2111
Molecular Weight: 520.589
Elemental Analysis: C, 71.52; H, 5.42; N, 10.76; O, 12.29
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
| 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/ |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 25.0 | 48.02 |
The following data is based on the product molecular weight 520.589 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.
| 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. |
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.
