(R)-Bicalutamide 是 Bicalutamide 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。

(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 [1] [2].

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 [1]. (R)-bicalutamide (0.02-20 μM) reduces na ve LNCaP cells survival in a dose-dependent manner [2]. Cell Proliferation Assay [2] 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 7 μM; 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 [3]. Animal Model: CD1 male nude (nu/nu) mice, with VCaP xenografts [3] Dosage: 10 mg/kg Administration: Orally gavage, daily, for 4 consecutive weeks Result: Suppressed tumor growth.

113299-40-4

C18H14F4N2O4S

430.37

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years