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Bicalutamide

比卡鲁胺,毕卡鲁胺,ICI-176334,ICI176334,ICI 176334,Casodex

Bicalutamide (比卡鲁胺; Casodex) 是口服的非甾体抗雄激素化合物，能与雄激素受体结合，可作用于前列腺癌，IC50为0.16 μM。

目录号
EY0665
EY0665
EY0665
纯度
99.41%
99.41%
99.41%
规格
10 mg
50 mg
100 mg
原价
220
450
680
售价
220
450
680
库存
现货
现货
现货
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  • 生物活性

    Bicalutamide is a nonsteroidal androgen receptor inhibitor useful in prostate cancer research. Bicalutamide induces cell death by a pathway that is independent of changes in mitochondrial membrane potential and Bcl-2 action. Displays peripheral selectivity and does not effect serum levels of LH and testosterone. Exhibits potent anticancer activity in vivo.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    0 nM-1 μM

  • 动物实验

    10 mg/kg 口服处理

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Clegg NJ, et al. Cancer Res. 2012, 72(6), 1494-1503.
    [2] A novel class of pyranocoumarin anti-androgen receptor signaling compounds: J. Guo, et al.; Mol. Cancer Ther. 6, 907 (2007)
    [3] Increased resistance to trail-induced apoptosis in prostate cancer cells selected in the presence of bicalutamide: M. Mitterberger, et al.; Prostate 67, 1194 (2007)
    [4] Interplay of nuclear factor-kappaB and B-myb in the negative regulation of androgen receptor expression by tumor necrosis factor alpha: S. Ko, et al.; Mol. Endocrinol. 22, 273 (2008)

    分子式
    C18H14F4N2O4S    		 分子量
    430.37    		 CAS号
    90357-06-5    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    86 mg/mL    		 Water
    Insoluble    		 Ethanol
    7 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT02487823 Non Castrate Metastatic Prostate Cancer Drug: BKM120 in combination with LH-RH agonists (suprefact) and bicalutamide Institut Paoli-Calmettes|Novartis Phase 1 2014-10-01 2017-03-01
    NCT02348281 Breast Cancer Drug: Bicalutamide Fudan University Phase 2 2015-01-01 2017-01-03
    NCT01044706 Healthy Drug: Bicalutamide Kremers Urban Development Company|Watson Pharmaceuticals Phase 1 2005-05-01 2010-02-28
    NCT03055312 Metastatic Triple Negative Breast Cancer Drug: TPC|Drug: Bicalutamide 150 mg Sun Yat-sen University Phase 3 2016-12-01 2017-02-22
    NCT00814788 Prostate Cancer Drug: bicalutamide|Drug: Everolimus University of California, Davis|Novartis Phase 2 2008-12-01 2016-01-07
    NCT00846976 Prostate Cancer Drug: Bicalutamide AstraZeneca Phase 3 1994-12-01 2015-01-20
    NCT00630344 Prostate Cancer Drug: RAD001|Drug: Bicalutamide Dana-Farber Cancer Institute|Beth Israel Deaconess Medical Center|Novartis Pharmaceuticals Phase 2 2008-02-01 2016-01-29
    NCT02353988 Breast Neoplasms Drug: Bicalutamide|Other: Physician's Choice Jinling Hospital, China|Wenzhou Medical University|The First People's Hospital of Lianyungang|Wuxi People's Hospital|Nanning Second People's Hospital|Jiangsu Province Hospital of Traditional Chinese Medicine|The Second Hospital of Nanjing Medical University Phase 2 2015-01-01 2015-02-02
    NCT00551044 Prostatic Neoplasms Drug: Bicalutamide Wirral University Teaching Hospital NHS Trust|AstraZeneca 2003-08-01 2007-10-29
    NCT02146937 Detectable Prostate Nodules Drug: Bicalutamide plus Finasteride- Combination therapy Sidney Kimmel Comprehensive Cancer Center Phase 2 2014-03-01 2017-03-20
    NCT00094328 Puberty, Precocious Drug: Bicalutamide|Drug: Anastrozole AstraZeneca Phase 2 2004-11-01 2017-02-14
    NCT02910050 Breast Cancer Drug: Bicalutamide|Drug: Aromatase Inhibitor Xu fei|Sun Yat-sen University Phase 2 2016-01-01 2016-09-20
    NCT02697032 Breast Cancer Drug: Bicalutamide|Procedure: FDHT PET University Medical Center Groningen Phase 2 2016-02-01 2016-11-24
    NCT01809691 Prostate Cancer Drug: TAK-700|Drug: Bicalutamide Southwest Oncology Group|Millennium Pharmaceuticals, Inc.|National Cancer Institute (NCI) Phase 3 2013-03-01 2017-02-23
    NCT01288911 Prostatic Neoplasms Drug: enzalutamide|Drug: Bicalutamide Astellas Pharma Inc|Medivation, Inc. Phase 2 2011-03-01 2016-09-22
    NCT01664923 Prostate Cancer Drug: Enzalutamide|Drug: Bicalutamide Medivation, Inc.|Astellas Pharma Inc Phase 2 2012-08-01 2016-12-20
    NCT00468715 Breast Cancer Drug: bicalutamide|Other: diagnostic laboratory biomarker analysis|Other: immunohistochemistry staining method Memorial Sloan Kettering Cancer Center|National Cancer Institute (NCI)|AstraZeneca Phase 2 2007-03-01 2016-04-28
    NCT00002874 Prostate Cancer Drug: bicalutamide|Radiation: low-LET cobalt-60 gamma ray therapy|Radiation: low-LET photon therapy Radiation Therapy Oncology Group|National Cancer Institute (NCI)|Southwest Oncology Group|NRG Oncology Phase 3 1998-02-01 2016-09-28

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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