(R)-Bicalutamide (Synonyms: (R)-比卡鲁胺)
目录号: PL01655 纯度: ≥99%
CAS No. :113299-40-4
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中文名称
(R)-Bicalutamide
中文别名
(R)-比卡鲁胺;(2R)-N-[4-氰基-3-三氟甲基苯基]-3-[(4-氟苯基)磺酰基]-2-羟基-2-甲基丙酰胺;(R)-(-)比卡鲁胺;(R)-(-)-比卡鲁胺-D4;5-氨基-3-三氟甲基吡唑;R-(-)-比卡鲁胺;R-比卡鲁胺(R)-Bicalutamide;R-比鲁卡胺;比卡鲁胺R-异构体
英文名称
(R)-Bicalutamide
英文别名
(R)-Bicalutamide;(2R)-N-[4-Cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide;R-Bicalutamide;ICI-187555;(R)-Casodex;R-BICALUTIMIDE;(R)-(-)-BICALUTAMIDE;BicalutaMide R-IsoMer;Bicalutamide impurity A;N-[4-Cyano-3-(Trifluoromethyl)Phenyl]-3-[(4-Flurophenyl)Thio]-2-Hydroxy-2-Methyl-Propanamide;(R)-N-[3-(Trifluoromethyl)-4-cyanophenyl]-2-methyl-2-hydroxy-3-(4-fluorophenylsulfonyl)propanamide;(2R)-N-[3-(Trifluoromethyl)-4-cyanophenyl]-2-methyl-2-hydroxy-3-(4-fluorophenylsulfonyl)propanamide
Cas No.
113299-40-4
分子式
C18H14F4N2O4S
分子量
430.37
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
(R)-Bicalutamide 是 Bicalutamide (HY-14249) 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。
生物活性
(R)-Bicalutamide is the (R)-enantiomer of Bicalutamide (HY-14249). (R)-Bicalutamide is an androgen receptor (AR) antagonist, with antineoplastic activity. (R)-Bicalutamide is widely used for the research of prostate cancer.
性状
Solid
IC50 & Target[1][2]
AR
体外研究(In Vitro)
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 manner.
has not independently confirmed the accuracy of these methods. They are for reference only.Cell Proliferation Assay
体内研究(In Vivo)
(R)-Bicalutamide (10 mg/kg; i.g.; daily; for 4 days) has antitumor efficacy in VCaP xenografts mice.
has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: CD1 male nude (nu/nu) mice
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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-
[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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (232.36 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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