FLTX1

SKU: orb1298469

Description

FLTX1 is a fluorescent Tamoxifen analog that specifically labels intracellular estrogen receptors in both permeabilized and live cells. It functions as a pure antiestrogen, inhibiting estrogen receptor activity in breast cancer research models without uterine agonist effects, making it valuable for imaging and mechanistic studies.

Research Area

Metabolism Research

Images & Validation

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Key Properties

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CAS Number	1481401-71-1
MW	520.58
Purity	98.46% (May vary between batches)
Formula	C₃₁H₂₈N₄O₄
SMILES	C(=C(/CC)\C1=CC=CC=C1)(\C2=CC=C(OCCN(C)C=3C=4C(C(N(=O)=O)=CC3)=NON4)C=C2)/C5=CC=CC=C5
Target	Estrogen/progestogen Receptor,Estrogen Receptor/ERR
Solubility	DMSO:5.21 mg/mL (10.01 mM)

Bioactivity

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Target IC50	ERα:87.5 nM
In Vivo	In vivo assays in mice revealed that unlike tamoxifen, FLTX1 was devoid of estrogenic uterotrophic effects, lacked of hyperplasic and hypertrophic effects, and failed to alter basal proliferating cell nuclear antigen immunoreactivity. 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. Read more...
In Vitro	Competition studies showed that FLTX1 binding was totally displaced by unlabeled tamoxifen and partially by estradiol, indicating the existence of non-ER-related triphenylethylene-binding sites. 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. FLTX1 lacked the strong agonistic effect of tamoxifen on ERα-dependent transcriptional activity. Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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FLTX1, FLTX 1, FLTX-1, ERR, fluorescent, ERα, Estrogen Receptor, estrogen, EstrogenReceptor, Estrogen Receptor/ERR, Inhibitor, inhibit, non-permeabilized, breast, antiestrogenic, cancer, progestogen Receptor, receptor, permeabilized, progestogenReceptor, Tamoxifen, uterus

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Compound Identifiers

PubChem CID

71816204 ↗

Key Properties

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No computed properties available.

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Purity:	>98% (HPLC)
CAS Number:	1481401-71-1
MW:	520.6
Formula:	C₃₁H₂₈N₄O₄

FLTX1

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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