Product Details
Product Name:
FLTX1 |
CAS No.:
1481401-71-1 |
Purity:
98.42% |
Supply Ability:
10g |
Release date:
2024/11/18 |
Product Introduction
Bioactivity
名称 | FLTX1 |
描述 | FLTX1 is a fluorescent derivative of Tamoxifen, designed to efficiently target and label intracellular Tamoxifen-binding sites (estrogen receptors) both under permeabilized and non-permeabilized conditions. Additionally, FLTX1 demonstrates strong antiestrogenic activity in breast cancer cells, resembling the potent antiestrogenic properties of Tamoxifen. Notably, FLTX1 does not exhibit any estrogenic agonistic effect on the uterus. |
体外活性 | 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[1]. |
体内活性 | 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[2]. |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 5.21 mg/mL (10 mM), Sonication is recommended.
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关键字 | FLTX1 | cancer | Estrogen Receptor/ERR | Inhibitor | fluorescent | Tamoxifen | antiestrogenic | inhibit | non-permeabilized | receptor | breast | FLTX 1 | estrogen | permeabilized | FLTX-1 | uterus |
相关产品 | Kaempferol | Tamoxifen | Mifepristone | Estradiol | Astragaloside IV | Estradiol benzoate | Cholesterol | Melatonin | Chrysin | Allura Red AC | Natamycin | Ethisterone |
相关库 | 核受体化合物库 | 经典已知活性库 | 抗乳腺癌化合物库 | 抗卵巢癌化合物库 | 内分泌激素分子库 | NO PAINS 化合物库 | 已知活性化合物库 | 抗癌化合物库 | 抗癌活性化合物库 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
Product name |
Price |
|
Suppliers |
Update time |
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$/ |
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Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |