切换导航

Bicalutamide

现货
Catalog No.
A5065
雄激素受体(Androgen receptor)拮抗剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 550.00
现货
100mg
¥ 500.00
现货

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

Background

Bicalutamide is an active non-steroidal androgen receptor antagonist with IC50 value of 160 nM.[1]
The androgen receptor (AR) is a type of nuclear receptor. It is activated by binding of either of dihydrotestosterone or the androgenic hormones testosterone. Then, it will translocate into the nucleus as DNA-binding transcription factor which regulates gene expression. Androgen is critical for the maintenance and development of the male sexual phenotype through related gene. The androgen receptor (AR) is also related to the core mechanism of castration-resistant prostate cancer.[1]
Bicalutamide inhibits growth in prostate cancer cells (VCaP cells) which overexpress androgen receptor by directly binding to AR then mediates androgen-mediated gene transcription with IC50 value of 160 nM. Bicalutamide directly binds to androgen receptor with Ki value of 12.5μM. In prostate cancer cells, bicalutamide impairs DNA binding and nuclear localization. Bicalutamide and MDV3100 significantly inhibited R1881-induced VP16-AR–mediated transcription in HepG2 cells with an IC50 value of 0.2 μM.[1] Bicalutamide has been an molecular template for designing selective androgen receptor antagonist used to the treatment of prostate cancer cells.[2] Bicalutamide also induces cell death by a different pathway which is independent of mitochondrial membrane potential changes and Bcl-2 action.[1]
Bicalutamide significantly inhibited AR then decrease the tumor growth in murine xenograft models, male immunodeficient mice which harbors LNCaP/AR-luc xenograft tumors.[1]
References:
[1].    Clegg NJ, Wongvipat J, Joseph JD, Tran C, Ouk S, Dilhas A, Chen Y, Grillot K, Bischoff ED, Cai L et al: ARN-509: a novel antiandrogen for prostate cancer treatment. Cancer Res 2012, 72(6):1494-1503.
[2].    Yin D, He Y, Perera MA, Hong SS, Marhefka C, Stourman N, Kirkovsky L, Miller DD, Dalton JT: Key structural features of nonsteroidal ligands for binding and activation of the androgen receptor. Mol Pharmacol 2003, 63(1):211-223.

文献引用

1. Bogner J, Zolghadr K, et al. "The fluorescent two-hybrid assay for live-cell profiling of androgen receptor modulators." J Steroid Biochem Mol Biol. 2016 May 9. PMID:27174722

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt430.37
Cas No.90357-06-5
FormulaC18H14F4N2O4S
Solubility≥21.5mg/mL in DMSO, ≥4.3 mg/mL in EtOH with ultrasonic, <2.57 mg/mL in H2O
Chemical NameN-[4-cyano-3-(trifluoromethyl)phenyl]-3-(4-fluorophenyl)sulfonyl-2-hydroxy-2-methylpropanamide
SDFDownload SDF
Canonical SMILESCC(CS(=O)(=O)C1=CC=C(C=C1)F)(C(=O)NC2=CC(=C(C=C2)C#N)C(F)(F)F)O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议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。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

VCaP 和 Hep-G2细胞系

溶解方法

在DMSO中的溶解度> 21.5 mg/ml。为了获得更高浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

10-11 ~10-4 M

应用

研究发现Bicalutamide能够抑制过表达雄激素受体的前列腺癌细胞(VCaP细胞)生长,其作用机制是直接结合AR,然后调控雄激素介导的基因转录。此外,Bicalutamide可以损伤前列腺癌细胞中的DNA结合和核定位。 在HepG2细胞中,Bicalutamide也可显著抑制R1881诱导的由VP16-AR介导的转录,其IC50值为0.2μM。

动物实验 [1]:

动物模型

携带LNCaP / AR-luc异种移植肿瘤的雄性免疫缺陷小鼠

剂量

10 mg/kg/day,口服

应用

在人类CRPC的临床有效的小鼠异种移植模型中,bicalutamide显示出比MDV3100更高的疗效。 在该模型中Bicalutamide于30mg/kg/d表现出最大治疗效果,而MDV3100显示出相同的疗效需要100mg / kg / d的剂量以及更高的稳态血浆浓度。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1] Clegg NJ, Wongvipat J, Joseph JD, Tran C, Ouk S, Dilhas A, Chen Y, Grillot K, Bischoff ED, Cai L et al: ARN-509: a novel antiandrogen for prostate cancer treatment. Cancer Res 2012, 72(6):1494-1503.

质量控制

化学结构

Bicalutamide

相关生物数据

Bicalutamide

相关生物数据

Bicalutamide