113299-40-4
中文名稱
(R)-比卡魯胺
英文名稱
(R)-Bicalutamide
CAS
113299-40-4
分子式
C18H14F4N2O4S
MDL 編號(hào)
MFCD00870866
分子量
430.37
MOL 文件
113299-40-4.mol
更新日期
2024/07/23 09:30:57
113299-40-4 結(jié)構(gòu)式
基本信息
中文別名
(2R)-N-[4-氰基-3-三氟甲基苯基]-3-[(4-氟苯基)磺酰基]-2-羥基-2-甲基丙酰胺(R)-比卡魯胺
英文別名
(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
(2R)-N-[3-(Trifluoromethyl)-4-cyanophenyl]-2-methyl-2-hydroxy-3-(4-fluorophenylsulfonyl)propanamide
(R)-N-[3-(Trifluoromethyl)-4-cyanophenyl]-2-methyl-2-hydroxy-3-(4-fluorophenylsulfonyl)propanamide
(R)-N-[4-Cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide
ICI-187555
物理化學(xué)性質(zhì)
熔點(diǎn)178-181°C
沸點(diǎn)650.3±55.0 °C(Predicted)
密度1.52±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C冷凍
溶解度可溶于丙酮（少許）、乙酸乙酯（少許）、甲醇（少許）
酸度系數(shù)(pKa)11.49±0.29(Predicted)
形態(tài)固體
顏色白色至灰白色
CAS 數(shù)據(jù)庫(kù)113299-40-4(CAS DataBase Reference)
(R)-比卡魯胺價(jià)格(試劑級(jí))
| 報(bào)價(jià)日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS號(hào) | 包裝 | 價(jià)格 |
| 2024/08/19 | HY-108250 | (R)-比卡魯胺 (R)-Bicalutamide | 113299-40-4 | 5mg | 900元 |
| 2024/08/19 | HY-108250 | (R)-比卡魯胺 (R)-Bicalutamide | 113299-40-4 | 10mM * 1mLin DMSO | 990元 |
| 2024/08/19 | HY-108250 | (R)-比卡魯胺 (R)-Bicalutamide | 113299-40-4 | 10mg | 1500元 |
常見(jiàn)問(wèn)題列表
生物活性
(R)-Bicalutamide 是 Bicalutamide (HY-14249) 的 R 型對(duì)映體。(R)-Bicalutamide 是一種雄激素受體 (AR) 拮抗劑，具有抗腫瘤活性。(R)-Bicalutamide 廣泛用于前列腺癌的研究。靶點(diǎn)
AR
體外研究
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 na?ve 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 na?ve LNCaP cells survival in a dose-dependent, with an IC 50 value of about 7μM; exerted a poor antiproliferative effect on LNCaP-Rbic. |
體內(nèi)研究
(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. |