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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 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)

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictogramsGHS hazard pictograms
GHS08,GHS09
警示詞危險(xiǎn)
危險(xiǎn)性描述H351-H360-H410
(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
2024/08/19HY-108250(R)-比卡魯胺
(R)-Bicalutamide
113299-40-45mg900元
2024/08/19HY-108250(R)-比卡魯胺
(R)-Bicalutamide
113299-40-410mM * 1mLin DMSO990元
2024/08/19HY-108250(R)-比卡魯胺
(R)-Bicalutamide
113299-40-410mg1500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.
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