Darolutamide NEW
| Price | $45 | $64 | $107 |
| Package | 1mg | 2mg | 5mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-05 |
Product Details
| Product Name: Darolutamide | CAS No.: 1297538-32-9 |
| Purity: 99.62% | Supply Ability: 10g |
| Release date: 2024/11/05 |
Product Introduction
Bioactivity
| 名稱 | Darolutamide |
| 描述 | Darolutamide (BAY-1841788) is an androgen receptor (AR) antagonist that blocks AR nuclear translocation (Ki: 11 nM). |
| 細(xì)胞實(shí)驗(yàn) | VCaP cells are treated with a submaximal concentration of mibolerone (0.1?nM) and increasing concentrations of test compounds in steroid-free assay medium supplemented with 4?mM GlutaMAX. After a 4-day incubation with the compounds, cell viability is measured using a WST-1 cell proliferation assay. To rule out non-AR –mediated toxicity, AR-negative PC cells (DU-145) and lung cancer cells (H1581) are treated with an increasing concentration of ODM-201, and cell viability is measured as described above.(Only for Reference) |
| 激酶實(shí)驗(yàn) | AR binding affinity: AR binding affinities of test compounds are studied in cytosolic lysates obtained from ventral prostates of castrated rats by a competition binding assay. Fresh prostates are minced and homogenized with Buffer A containing protease inhibitors. The homogenates are centrifuged and the resultant supernatants are treated with a dextran-coated charcoal solution to remove endogenous steroids. The dissociation constant of the radio ligand [3H]mibolerone for isolated rat ARs is determined in a saturation binding experiment. For the determination of Ki values, prostate cytosol preparations and 1?nM [3H]mibolerone are incubated with increasing concentrations of test compounds overnight. After the incubation, bound and free steroids are separated by treatment with 100?μL of dextran-coated charcoal suspension. Bound radioactivity is determined by counting 100?μL of supernatant fraction in 200?μL of scintillation fluid using a microbeta counter. All procedures are carried out at 0–4?°C. |
| 體外活性 | In AR-HEK293 cells stably expressing full-length hAR, ODM-201 inhibits human AR (hAR) with IC50 of 26 nM. ODM-201 inhibits VCaP cell proliferation with IC50 of 230 nM, while has no effect on the viability of AR-negative cell lines tested, DU-145 prostate cancer cells and H1581 lung cancer cells. [1] |
| 體內(nèi)活性 | In mice bearing VCaP xenografts, ODM-201 (50?mg/kg, p.o.) significantly inhibits castration-resistant prostate tumor growth. [1] |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 70 mg/mL (175.5 mM) Ethanol : 36 mg/mL (90.3 mM) H2O : < 1 mg/mL (insoluble or slightly soluble) |
| 關(guān)鍵字 | Inhibitor | Darolutamide | Androgen Receptor | ODM201 | inhibit | BAY1841788 | ODM 201 | BAY 1841788 |
| 相關(guān)產(chǎn)品 | Dehydroisoandrosterone 3-acetate | Bicalutamide | 2,2,5,7,8-Pentamethyl-6-Chromanol | S-23 | Bavdegalutamide | Enzalutamide | Adrenosterone | Allura Red AC | SK33 | Sunset Yellow FCF | Ostarine | Flutamide |
| 相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | EMA 上市藥物庫(kù) | 抗癌臨床化合物庫(kù) | 藥物功能重定位化合物庫(kù) | 抑制劑庫(kù) | FDA 上市藥物庫(kù) | 抗癌上市藥物庫(kù) | 已知活性化合物庫(kù) | 抗癌活性化合物庫(kù) | 抗癌藥物庫(kù) |
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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United States- Since: 2011-01-07
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