Product Details
| Product Name:
Brilanestrant |
CAS No.:
1365888-06-7 |
| Purity:
98.71% |
Supply Ability:
10g |
| Release date:
2024/11/14 |
Product Introduction
Bioactivity
| 名稱 | Brilanestrant |
| 描述 | Brilanestrant (GDC-0810) is a selective estrogen receptor degrader (IC50: 0.7 nM). |
| 細(xì)胞實驗 | MCF-7 cells are adjusted to a concentration of 40000 cells per mL in RPMI containing 10% FBS and 20 mM HEPES. Then 16 μL of the cell suspension (640 cells) is added to each well of a 384-well plate, and the cells are incubated overnight to allow the cells to adhere. The following day a 10-point, serial 1:5 dilution of each compound is added to the cells in 16 μL at a final concentration ranging from 10 to 0.000005 μM. After 5 days' compound exposure, 16 μL of CellTiter-GLo is added to the cells, and the relative luminescence units of each well are determined. CellTiter-GLo added to 32 μL of medium without cells is used to obtain a background value. The percent viability of each sample is determined as follows: RLU sample-RLU background/RLU untreated cells-RLU background ×100=%viability. |
| 動物實驗 | Time release pellets containing 0.72 mg 17-β estradiol are subcutaneously implanted into nu/nu mice. MCF-7 cells are grown in RPMI containing 10% FBS at 5% CO2 37°C. Trypsinized cells are pelleted and resuspended in 50% RPMI（serum free）and 50% Matrigel at 1×107 cells/mL. MCF-7 cells are subcutaneously injected (100 μL/animal) on the right flank 2-3 days post pellet implantation. Tumor volume (length × width2/2) is monitored biweekly. When tumors reach an average volume of appr 200 mm3 animals are randomized and treatment is started. Animals are treated with vehicle or compound daily for 4 weeks. Tumor volume and body weight are monitored biweekly throughout the study. |
| 體外活性 | Brilanestrant is a ERα binder (IC50: 6.1 nM), a full transcriptional antagonist with no agonism (3× ERE, IC50: 2 nM), and displays good potency and efficacy in ER-α degradation (EC50: 0.7 nM) and MCF-7 breast cancer cell viability (IC50; 2.5 nM) assays [1]. Brilanestrant induces a distinct ERα conformation versus tamoxifen and other ER therapeutics, and does not exhibit tamoxifen-like ER agonism in MCF7 cells [2]. |
| 體內(nèi)活性 | The pharmacokinetic profile of Brilanestrant shows it is a clearance molecule across species, with good bioavailability (40%-60%). Brilanestrant (3 mg/kg, p.o.) shows substantial tumor-growth inhibition in a tamoxifen-sensitive MCF-7 xenograft model, while at the highest dose of 100 mg/kg/day, all animals show tumor regression of more than 50% without weight loss [1]. Brilanestrant exhibits low clearance (11 mL/min/kg) and 61% oral bioavailability. Brilanestrant (1-100 mg/kg/day, p.o.) displays dose-dependent efficacy in the MCF7 xenograft model [2]. |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 55 mg/mL (123.07 mM)
H2O : Insoluble
|
| 關(guān)鍵字 | inhibit | ARN810 | Estrogen Receptor/ERR | RG6046 | Inhibitor | Brilanestrant | RG-6046 | ARN 810 |
| 相關(guān)產(chǎn)品 | Kaempferol | Tamoxifen | Mifepristone | Estradiol | Astragaloside IV | Estradiol benzoate | Cholesterol | Melatonin | Chrysin | Allura Red AC | Natamycin | Ethisterone |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | 抗癌臨床化合物庫 | 藥物功能重定位化合物庫 | 內(nèi)分泌激素分子庫 | 口服活性化合物庫 | 臨床期小分子藥物庫 | 已知活性化合物庫 | 抗癌化合物庫 | 抗癌活性化合物庫 | 抗癌藥物庫 |
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
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Anhui Ruihan Technology Co., Ltd
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2023-08-21 |
United States