2,1,3-Benzoxadiazol-4-amine, N-[2-[4-[(1Z)-1,2-diphenyl-1-buten-1-yl]phenoxy]ethyl]-N-methyl-7-nitro-
- CAS No.
- 1481401-71-1
- Chemical Name:
- 2,1,3-Benzoxadiazol-4-amine, N-[2-[4-[(1Z)-1,2-diphenyl-1-buten-1-yl]phenoxy]ethyl]-N-methyl-7-nitro-
- Synonyms
- FLTX1;CB38231393;FLTX1, 10 mM in DMSO;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-;(Z)-N-(2-(4-(1,2-Diphenylbut-1-en-1-yl)phenoxy)ethyl)-N-methyl-7-nitrobenzo[c][1,2,5]oxadiazol-4-amine;cancer,Estrogen Receptor/ERR,FLTX1,FLTX 1,Inhibitor,fluorescent,Tamoxifen,antiestrogenic,inhibit,non-permeabilized,receptor,breast,FLTX-1,estrogen,permeabilized,uterus
- CBNumber:
- CB38231393
- Molecular Formula:
- C31H28N4O4
- Molecular Weight:
- 520.58
- MDL Number:
- MOL File:
- 1481401-71-1.mol
2,1,3-Benzoxadiazol-4-amine, N-[2-[4-[(1Z)-1,2-diphenyl-1-buten-1-yl]phenoxy]ethyl]-N-methyl-7-nitro- Chemical Properties,Uses,Production
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
2,1,3-Benzoxadiazol-4-amine, N-[2-[4-[(1Z)-1,2-diphenyl-1-buten-1-yl]phenoxy]ethyl]-N-methyl-7-nitro- Preparation Products And Raw materials
Raw materials
Preparation Products
2,1,3-Benzoxadiazol-4-amine, N-[2-[4-[(1Z)-1,2-diphenyl-1-buten-1-yl]phenoxy]ethyl]-N-methyl-7-nitro- Suppliers
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