(R)-比卡鲁胺
| 中文名称 | (R)-比卡鲁胺 |
|---|---|
| 中文同义词 | (2R)-N-[4-氰基-3-三氟甲基苯基]-3-[(4-氟苯基)磺酰基]-2-羟基-2-甲基丙酰胺;(R)-比卡鲁胺;比卡鲁胺R-异构体;R-比鲁卡胺;化合物 (R)-BICALUTAMIDE |
| 英文名称 | (R)-Bicalutamide |
| 英文同义词 | (R)-(-)-BICALUTAMIDE;(R)-BICALUTAMIDE;N-[4-Cyano-3-(Trifluoromethyl)Phenyl]-3-[(4-Flurophenyl)Thio]-2-Hydroxy-2-Methyl-Propanamide;R-BICALUTIMIDE;(R)-Casodex;Propanamide, N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methyl-, (2R)-;Propanamide, N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methyl-, (R)-;(2R)-N-[4-Cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide |
| CAS号 | 113299-40-4 |
| 分子式 | C18H14F4N2O4S |
| 分子量 | 430.37 |
| EINECS号 | 692-949-8 |
| 相关类别 | 泌尿系统药物;医药与生物化工;Sulfur & Selenium Compounds;Chiral Reagents;Intermediates & Fine Chemicals;Pharmaceuticals |
| Mol文件 | 113299-40-4.mol |
| 结构式 |  |
(R)-比卡鲁胺 性质
| 熔点 | 178-181°C |
|---|---|
| 沸点 | 650.3±55.0 °C(Predicted) |
| 密度 | 1.52±0.1 g/cm3(Predicted) |
| 储存条件 | -20°C Freezer |
| 溶解度 | 可溶于丙酮（少许）、乙酸乙酯（少许）、甲醇（少许） |
| 形态 | 固体 |
| 酸度系数(pKa) | 11.49±0.29(Predicted) |
| 颜色 | 白色至类白色 |
| CAS 数据库 | 113299-40-4(CAS DataBase Reference) |
(R)-Bicalutamide 是 Bicalutamide (HY-14249) 的 R 型对映体。(R)-Bicalutamide 是一种雄激素受体 (AR) 拮抗剂，具有抗肿瘤活性。(R)-Bicalutamide 广泛用于前列腺癌的研究。
AR
Bicalutamide (HY-14249) is available as a racemic mixture. The R isomer (R-bicalutamide) has an ≈30-fold higher binding affinity to the AR than the S isomer.
(R)-bicalutamide (0.02-20 μM) reduces naïve LNCaP cells survival in a dose-dependent.
Cell Proliferation Assay
| Cell Line: | LNCaP cells, LNCaP-Rbic cells |
| Concentration: | 0.02 μM, 0.2 μM, 2 μM, 20 μM |
| Incubation Time: | 144 hours |
| Result: | Reduced naïve LNCaP cells survival in a dose-dependent, with an IC 50 value of about 7μM; exerted a poor antiproliferative effect on LNCaP-Rbic. |
(R)-Bicalutamide (10 mg/kg; i.g.; daily; for 4 days) has antitumor efficacy in VCaP xenografts mice.
| Animal Model: | CD1 male nude (nu/nu) mice, with VCaP xenografts |
| Dosage: | 10 mg/kg |
| Administration: | Orally gavage, daily, for 4 consecutive weeks |
| Result: | Suppressed tumor growth. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-108250 | (R)-比卡鲁胺 (R)-Bicalutamide | 113299-40-4 | 5mg | 900元 |
| 2024/01/25 | HY-108250 | (R)-比卡鲁胺 (R)-Bicalutamide | 113299-40-4 | 10mM * 1mLin DMSO | 990元 |