Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Darolutamide (BAY-1841788) 是一种雄激素受体(AR) 拮抗剂,在体内试验中的IC50值为26 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 233 | 现货 | ||
2 mg | ¥ 328 | 现货 | ||
5 mg | ¥ 690 | 现货 | ||
10 mg | ¥ 1,120 | 现货 | ||
25 mg | ¥ 1,890 | 现货 | ||
50 mg | ¥ 2,820 | 现货 | ||
100 mg | ¥ 4,570 | 现货 | ||
500 mg | ¥ 9,520 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 776 | 现货 |
产品描述 | Darolutamide (BAY-1841788) is an androgen receptor (AR) antagonist that blocks AR nuclear translocation (Ki: 11 nM). |
靶点活性 | Androgen receptor:11 nM(Ki) |
体外活性 | 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] |
体内活性 | In mice bearing VCaP xenografts, ODM-201 (50?mg/kg, p.o.) significantly inhibits castration-resistant prostate tumor growth. [1] |
激酶实验 | 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. |
细胞实验 | 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) |
别名 | ODM-201, BAY-1841788 |
分子量 | 398.85 |
分子式 | C19H19ClN6O2 |
CAS No. | 1297538-32-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 74 mg/mL (185.5 mM)
Ethanol: 36 mg/mL (90.3 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.5072 mL | 12.536 mL | 25.0721 mL | 62.6802 mL |
5 mM | 0.5014 mL | 2.5072 mL | 5.0144 mL | 12.536 mL | |
10 mM | 0.2507 mL | 1.2536 mL | 2.5072 mL | 6.268 mL | |
20 mM | 0.1254 mL | 0.6268 mL | 1.2536 mL | 3.134 mL | |
50 mM | 0.0501 mL | 0.2507 mL | 0.5014 mL | 1.2536 mL | |
DMSO | 100 mM | 0.0251 mL | 0.1254 mL | 0.2507 mL | 0.6268 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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