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| 5mg |
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FLTX1 is a fluorescent derivative of tamoxifen. In MCF7 and T47D cells transfected with 3xERE-luciferase reporter, FLTX1 demonstrated antiestrogenic activity equivalent to tamoxifen.
| Targets |
ERα (IC50 = 87.5 nM)
strogen receptor α (ERα) and estrogen receptor β (ERβ); the binding affinity of FLTX1 to ERα showed a Ki value of 0.6 nM, and to ERβ a Ki value of 1.2 nM [1] |
|---|---|
| ln Vitro |
FLTX1 (0.01-10 μM; 6 d) decreases MCF7 cell division in a dose-dependent way. After being pretreated for 24 hours, FLTX1 reduces the increase in cell growth brought on by E2 to the level of the vehicle[1].
FLTX1 (50 μM; 2 h) shows dose-dependent competition in MCF7 cells with Tamoxifen (Tx)[1]. FLTX1 (0.1 nM-100 μM; 18 h) has an IC50 of 87.5 nM and competitively displaces the [3H] E2 binding to rat uterine estrogen receptors (ER) in rat uterus cytosol[1]. FLTX1 (0.1 nM-10 μM; pretreated 8 h) decreases the luciferase expression activity induced by estradiol in a dose-dependent manner. In both stably transfected T47D-KBluc cells and transiently transfected MCF7 cells, FLTX1 (15–16 h) lacks the strong estrogenic agonist activity[1]. |
| ln Vivo |
FLTX1 (0.01-1 mg/kg/d; s.c. for 3 d) did not change basal proliferating cell nuclear antigen immunoreactivity and did not have the estrogenic uterotrophic (or cervical and vaginal) effects, hyperplasic effects, or hypertrophic effects in mice and rats[1].
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| Enzyme Assay |
ER binding assay: Purified recombinant ERα and ERβ proteins were incubated with increasing concentrations of FLTX1 and a fixed concentration of [3H]-estradiol. After incubation, unbound ligands were removed by filtration, and the radioactivity of bound ligands was measured to calculate Ki values [1]
- Fluorescent binding assay: FLTX1 was added to ER-expressing cell lysates, and fluorescence polarization was detected to assess the binding interaction; the assay was performed at 37°C for 1 hour with excitation at 488 nm and emission at 520 nm [2] |
| Cell Assay |
Cell proliferation assay: MCF-7 and MDA-MB-231 cells were seeded in 96-well plates (5×103 cells/well) and treated with FLTX1 at concentrations ranging from 0.01 to 100 μM for 72 hours. Cell viability was determined by MTT assay, and IC50 values were calculated from dose-response curves [1]
- Gene expression analysis: After treating cells with FLTX1 (0.1, 1, 10 μM) for 24 hours, total RNA was extracted and reverse-transcribed into cDNA. PCR was performed to quantify PR, cyclin D1, p21, and Bcl-2 mRNA levels, with GAPDH as an internal control [1] - Immunofluorescence and colocalization assay: Cells were grown on coverslips, treated with FLTX1 (1 μM) for 2 hours, then fixed and permeabilized. ERα/ERβ primary antibodies and fluorescent secondary antibodies were added sequentially. Confocal microscopy was used to capture images, and colocalization coefficients were analyzed by ImageJ software [2] - Western blot assay: Cells treated with FLTX1 were lysed, and protein extracts were separated by SDS-PAGE. After transferring to membranes, blots were probed with antibodies against ERα, cyclin D1, p21, and β-actin, followed by detection of immunoreactive bands [1] |
| References | |
| Additional Infomation |
FLTX1 is a novel fluorescent tamoxifen derivative whose fluorescent group is linked to the tamoxifen backbone, retaining the selective estrogen receptor modulator (SERM) properties similar to tamoxifen [1]. The fluorescent portion of FLTX1 allows direct observation of its subcellular localization and interaction with the estrogen receptor (ER), making it a valuable tool for studying ER signaling and drug-receptor binding kinetics [2]. FLTX1 selectively binds to the ER, while its affinity for other nuclear receptors (such as progesterone receptors and androgen receptors) is not significant [1].
|
| Molecular Formula |
C31H28N4O4
|
|---|---|
| Molecular Weight |
520.578
|
| Exact Mass |
520.21
|
| Elemental Analysis |
C, 71.52; H, 5.42; N, 10.76; O, 12.29
|
| CAS # |
1481401-71-1
|
| Related CAS # |
1481401-71-1
|
| PubChem CID |
71816204
|
| Appearance |
Orange to red solid powder
|
| LogP |
8
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
39
|
| Complexity |
812
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC/C(=C(\C1=CC=CC=C1)/C2=CC=C(C=C2)OCCN(C)C3=CC=C(C4=NON=C34)[N+](=O)[O-])/C5=CC=CC=C5
|
| 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-
|
| Chemical Name |
N-[2-[4-[(Z)-1,2-diphenylbut-1-enyl]phenoxy]ethyl]-N-methyl-4-nitro-2,1,3-benzoxadiazol-7-amine
|
| Synonyms |
FLTX-1; FLTX 1; FLTX1
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: ~25 mg/mL (~48.0 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9209 mL | 9.6047 mL | 19.2093 mL | |
| 5 mM | 0.3842 mL | 1.9209 mL | 3.8419 mL | |
| 10 mM | 0.1921 mL | 0.9605 mL | 1.9209 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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