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Bicalutamide

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Chemical Structure| 90357-06-5 同义名 : 毕卡鲁胺 ;ICI 176334;ZD 176334;Abbreviation: CDX. US brand name: Casodex. Foreign brand name: Cosudex.
CAS号 : 90357-06-5
货号 : A176397
分子式 : C18H14F4N2O4S
纯度 : 99%
分子量 : 430.373
MDL号 : MFCD00869971
存储条件：

粉末 Keep in dark place,Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(116.18 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+40% PEG300+water 2.2 mg/mL clear

PO 0.5% CMC-Na 26 mg/mL suspension

生物活性
靶点

  • Androgen Receptor

    Androgen Receptor, IC50:0.16 μM
描述 The androgen receptor (AR) and the androgen-AR signaling pathway play a significant role in male sexual differentiation and the development and function of male reproductive and non-reproductive organs [7]. Bicalutamide is an AR antagonist with IC50 of 0.16 μM in LNCaP/AR(cs) cell lines. In the setting of Castration-resistant prostate cancer (CRPC), bicalutamide undergoes an antagonist-to-agonist switch, stimulating AR activity and prostate tumor cell growth. In addition, bicalutamide stimulate proliferation of VCaP cells in a dose-dependent manner. The therapeutic effect of bicalutamide (10 mg/kg/d) was conducted in castrate mice bearing LNCaP/AR(cs) xenograft tumors, the antitumor activity of bicalutamide in this model was largely restricted to growth inhibition rather than tumor shrinkage [8]. Notably, Single administration of bicalutamide reduced tumor growth by 79% at defined submaximal doses [9].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
CHO-K1 cells Function assay 2 h Displacement of [3H]mibolerone from human AR expressed in CHO-K1 cells after 2 hrs by scintillation counting, IC50=0.2 μM 20381361
COS1 cells Function assay Antagonist activity against pSG5-tagged human androgen receptor expressed in COS1 cells assessed as reduction in receptor-mediated transcriptional activity by AR-regulated rat probasin promoter fragment driven firefly luciferase reporter assay, IC50=0.0869 μM 25646649
COS7 cells Function assay Agonist activity at human androgen receptor W741C mutant expressed in COS7 cells assessed as luciferase activity after 24 hrs by reporter gene assay, EC50=0.18 μM 22094279
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00298155 Cancer Prosta... 展开 >>te Neoplasms 收起 << Phase 2 Completed - United States, Washington ... 展开 >> Veterans' Administration Puget Sound Health Care System (VAPSHCS) Seattle, Washington, United States, 98108-1532 University of Washington Seattle, Washington, United States, 98195-6158 收起 <<
NCT00298155 - Completed - -
NCT02064036 Adenocarcinoma of the Prostate Not Applicable Recruiting October 2018 United States, California ... 展开 >> UC Davis Sacramento Cancer Center Dept of Radiation Oncology Recruiting Sacramento, California, United States, 95817 Contact: Richard Valicenti, MD    916-724-8295    rkvalicenti@ucdavis.edu    Principal Investigator: Richard Valicenti, MD 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.32mL

0.46mL

0.23mL

11.62mL

2.32mL

1.16mL

23.24mL

4.65mL

2.32mL
参考文献

[1]The Protective Role Of Ascorbic Acid Administration On The Bicalutamide Induced Reduction In Semen Quality In The Sprague - Dawley Rat

[2]Cockshott ID, Plummer GF, et al. The pharmacokinetics of Casodex in laboratory animals. Xenobiotica. 1991 Oct;21(10):1347-55.

[3]Attar RM, Jure-Kunkel M, et al. Discovery of BMS-641988, a novel and potent inhibitor of androgen receptor signaling for the treatment of prostate cancer. Cancer Res. 2009 Aug 15;69(16):6522-30.

[4]Sirotnak FM, She Y, et al. Studies with CWR22 xenografts in nude mice suggest that ZD1839 may have a role in the treatment of both androgen-dependent and androgen-independent human prostate cancer. Clin Cancer Res. 2002 Dec;8(12):3870-6.

[5]Shukla GC, Plaga AR, Shankar E, Gupta S. Androgen receptor-related diseases: what do we know? Andrology. 2016 May;4(3):366-81. doi: 10.1111/andr.12167. Epub 2016 Mar 16. PMID: 26991422.

[6]Clegg NJ, Wongvipat J, Joseph JD, Tran C, Ouk S, Dilhas A, Chen Y, Grillot K, Bischoff ED, Cai L, Aparicio A, Dorow S, Arora V, Shao G, Qian J, Zhao H, Yang G, Cao C, Sensintaffar J, Wasielewska T, Herbert MR, Bonnefous C, Darimont B, Scher HI, Smith-Jones P, Klang M, Smith ND, De Stanchina E, Wu N, Ouerfelli O, Rix PJ, Heyman RA, Jung ME, Sawyers CL, Hager JH. ARN-509: a novel antiandrogen for prostate cancer treatment. Cancer Res. 2012 Mar 15;72(6):1494-503. doi: 10.1158/0008-5472.CAN-11-3948. Epub 2012 Jan 20. PMID: 22266222; PMCID: PMC3306502.

[7]Squillace RM, Miller D, Wardwell SD, Wang F, Clackson T, Rivera VM. Synergistic activity of the mTOR inhibitor ridaforolimus and the antiandrogen bicalutamide in prostate cancer models. Int J Oncol. 2012 Aug;41(2):425-32. doi: 10.3892/ijo.2012.1487. Epub 2012 May 18. PMID: 22614157; PMCID: PMC3582879.