(R)-Bicalutamide is the (R)-enantiomer of Bicalutamide . (R)-Bicalutamide is an androgen receptor (AR) antagonist, with antineoplastic activity. (R)-Bicalutamide is widely used for the research of prostate cancer.
IC50&Target
AR
体外研究
Bicalutamide 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 manner.
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 IC50 value of about 7 μM; exerted a poor antiproliferative effect on LNCaP-Rbic.
体内研究
(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.
分子式
C18H14F4N2O4S
分子量
430.37
CAS号
113299-40-4
中文名称
(R)-比卡鲁胺
运输条件
Room temperature in continental US; may vary elsewhere.