Synonym
FLTX1; FLTX-1; FLTX 1; CB-38231393; CB38231393; CB 38231393;
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-]
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 |
mg/mL |
mM |
Solubility |
DMSO |
25.0 |
48.02 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
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.
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: 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.
2: 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.
3: 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.
4: Díaz M, Lobo F, Hernández D, Amesty Á, Valdés-Baizabal C, Canerina-Amaro A,
Mesa-Herrera F, Soler K, Boto A, Marín R, Estévez-Braun A, Lahoz F.
FLTX2: A Novel Tamoxifen Derivative Endowed with Antiestrogenic,
Fluorescent, and Photosensitizer Properties. Int J Mol Sci. 2021 May
19;22(10):5339. doi: 10.3390/ijms22105339. PMID: 34069498; PMCID: PMC8161337.