| 中文名称 | (R)-比卡鲁胺 |
| 英文名称 | (R)-Bicalutamide |
| CAS号 | 113299-40-4 |
| 分子式 | C18H14F4N2O4S |
| 分子量 | 430.37 |
| EINECS号 | 692-949-8 |
| 熔点 | 178-181°C |
| 沸点 | 650.3±55.0 °C(Predicted) |
| 密度 | 1.52±0.1 g/cm3(Predicted) |
| 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 |
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. |