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  • (R)-Bicalutamide
(R)-Bicalutamide的可视化放大

(R)-Bicalutamide

(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。

原价
¥987-1625
价格
790-1300
(R)-Bicalutamide的二维码

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  • 库存: 现货
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  • 货号: ajcx31876
  • CAS: 113299-40-4
  • 别名: (R)-比卡鲁胺
  • 分子式: C18H14F4N2O4S
  • 分子量: 430.37
  • 纯度: >98%
  • 溶解度: DMSO: 100 mg/mL (232.36 mM)
  • 储存: Store at -20°C
  • 库存: 现货

Background

(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[2]. Cell Proliferation Assay[2] Cell Line: LNCaP cells, LNCaP-Rbic cells


(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]


[1]. Hongli Liu, et al. Molecular mechanism of R-bicalutamide switching from androgen receptor antagonist to agonist induced by amino acid mutations using molecular dynamics simulations and free energy calculation. J Comput Aided Mol Des. 2016 Dec;30(12):1189-1200. [2]. Sara Pignatta, et al. Prolonged exposure to (R)-bicalutamide generates a LNCaP subclone with alteration of mitochondrial genome. Mol Cell Endocrinol. 2014 Jan 25;382(1):314-324. [3]. Anna Tesei, et al. Effect of Small Molecules Modulating Androgen Receptor (SARMs) in Human Prostate Cancer Models. PLoS One. 2013; 8(5): e62657.

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