| Identification | Back Directory | [Name]
2,1,3-Benzoxadiazol-4-amine, N-[2-[4-[(1Z)-1,2-diphenyl-1-buten-1-yl]phenoxy]ethyl]-N-methyl-7-nitro- | [CAS]
1481401-71-1 | [Synonyms]
FLTX1
1481401-71-1
N-(7-Nitrobenzo[c][1,2,5]oxadiazol-4-yl)demethyltamoxifen
N-(7-Nitrobenzo[c][1,2,5]oxadiazol-4-
yl)demethyltamoxife
2,1,3-Benzoxadiazol-4-amine, N-[2-[4-[(1Z)-1,2-diphenyl-1-buten-1-yl]phenoxy]ethyl]-N-methyl-7-nitro- | [Molecular Formula]
C31H28N4O4 | [MOL File]
1481401-71-1.mol | [Molecular Weight]
520.58 |
| Chemical Properties | Back Directory | [Boiling point ]
679.5±65.0 °C(Predicted) | [density ]
1.258±0.06 g/cm3(Predicted) | [solubility ]
DMSO : 25 mg/mL (48.02 mM; Need ultrasonic) | [form ]
Solid | [pka]
-3.81±0.50(Predicted) | [color ]
Orange to red |
| Hazard Information | Back Directory | [Uses]
FLTX1 is 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[1][2]. | [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[1]. | [IC 50]
ERα: 87.5 nM (IC50) | [References]
[1] Marrero-Alonso J, et, al. 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
[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. DOI:10.1007/978-1-4939-3127-9_13 |
|
|