ARN-509

Apalutamide

ARN-509是一种选择性的,竞争性的androgen receptor抑制剂,IC50为16 nM,有效治疗前列腺癌。

目录号
EY1388
EY1388
EY1388
EY1388
纯度
99.62%
99.62%
99.62%
99.62%
规格
1 mg
5 mg
10 mg
50 mg
原价
340
799
1200
3100
售价
340
799
1200
3100
库存
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    ARN-509 is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM in a cell-free assay, useful for prostate cancer treatment.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    10 μM

  • 动物实验

    30 mg/kg/天口服

  • 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 AKm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.

    分子式
    C21H15F4N5O2S
    分子量
    477.43
    CAS号
    956104-40-8
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    20 mg/mL
    Water
    <1 mg/mL
    Ethanol
    5 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
    NCT01822041 Healthy Drug: ARN-509 Aragon Pharmaceuticals, Inc. Phase 1 2013-03-01 2013-09-12
    NCT02721979 Stage II Prostate Adenocarcinoma Drug: Androgen Receptor Antagonist ARN-509|Other: Laboratory Biomarker Analysis|Other: Quality-of-Life Assessment University of Washington|National Cancer Institute (NCI)|Janssen Scientific Affairs, LLC Phase 2 2017-06-01 2017-03-23
    NCT02770391 Prostate Cancer Drug: Leuprolide acetate|Drug: ARN-509|Procedure: Radical prostatectomy Case Comprehensive Cancer Center Phase 2 2016-10-01 2016-12-12
    NCT01171898 Prostate Cancer Drug: ARN-509 (Phase 1)|Drug: ARN-509 (Phase 2) Aragon Pharmaceuticals, Inc. Phase 1|Phase 2 2010-07-26 2017-03-16
    NCT01792687 Prostate Cancer Drug: ARN-509|Drug: Abiraterone acetate|Drug: Prednisone Aragon Pharmaceuticals, Inc. Phase 1 2013-02-01 2017-03-01
    NCT02849990 Stage III Prostate Adenocarcinoma|Stage III Prostate Cancer|Stage IV Prostate Adenocarcinoma|Stage IV Prostate Cancer Drug: Abiraterone Acetate|Drug: Androgen Receptor Antagonist ARN-509|Drug: Degarelix|Drug: Indomethacin|Other: Laboratory Biomarker Analysis|Drug: Prednisone University of Washington|National Cancer Institute (NCI)|Janssen Scientific Affairs, LLC Phase 2 2017-04-15 2017-03-09
    NCT03080116 Prostate Cancer|Neoadjuvant Therapy|Androgen Antagonists|Prostatectomy Drug: ARN-509|Drug: Degarelix|Other: Placebo Universitaire Ziekenhuizen Leuven Phase 2 2017-04-30 2017-03-08
    NCT01790126 Prostate Cancer Drug: ARN-509|Drug: LHRH Agonist Aragon Pharmaceuticals, Inc. Phase 2 2013-03-01 2017-03-17
    NCT02949284 Stage II Prostate Adenocarcinoma|Stage III Prostate Adenocarcinoma Drug: Abiraterone Acetate|Drug: Androgen Receptor Antagonist ARN-509|Biological: Gonadotropin-releasing Hormone Analog|Drug: Prednisone|Other: Quality-of-Life Assessment|Other: Questionnaire Administration|Procedure: Radical Prostatectomy Rutgers, The State University of New Jersey|National Cancer Institute (NCI) Phase 2 2017-06-01 2017-02-03
    NCT01946204 Prostatic Neoplasms Drug: Apalutamide|Drug: Placebo Aragon Pharmaceuticals, Inc. Phase 3 2013-10-01 2017-02-17
    NCT02578797 Castration-Resistant Prostate Cancer Drug: Apalutamide Aragon Pharmaceuticals, Inc. Phase 1 2015-12-01 2017-03-02
    NCT02123758 Prostatic Neoplasms|Metastatic Castration-Resistant Prostate Cancer (mCRPC) Drug: Abiraterone Acetate|Drug: Prednisone|Drug: JNJ-56021927 Aragon Pharmaceuticals, Inc. Phase 1 2014-07-09 2017-03-08
    NCT02489318 Prostate Cancer Drug: Apalutamide|Drug: Placebo|Drug: Androgen Deprivation Therapy (ADT) Aragon Pharmaceuticals, Inc. Phase 3 2015-11-27 2017-03-09
    NCT02772588 Prostate Cancer Drug: ARN-509|Drug: Abiraterone|Drug: Leuprolide|Radiation: stereotactic, ultra-fractionated radiotherapy Memorial Sloan Kettering Cancer Center|Janssen Pharmaceuticals|Weill Medical College of Cornell University|University of Michigan Phase 2 2016-05-01 2016-12-12
    NCT02106507 Prostate Cancer Drug: apalutamide|Drug: Everolimus Memorial Sloan Kettering Cancer Center|Aragon Pharmaceuticals, Inc. Phase 1 2014-04-01 2016-12-27
    NCT02703623 Prostate Cancer Drug: Abiraterone acetate|Drug: Prednisone|Drug: ARN509|Drug: Ipilimumab|Drug: Cabazitaxel|Drug: Carboplatin M.D. Anderson Cancer Center|Bristol-Myers Squibb|Janssen, LP|Sanofi Phase 2 2016-05-01 2017-03-01
    NCT02031666 Healthy Drug: JNJ-56021927 capsule|Drug: JNJ-56021927 tablet Aragon Pharmaceuticals, Inc. Phase 1 2013-12-01 2016-10-19
    NCT02160756 Healthy Drug: JNJ-56021927 Softgel Capsule|Drug: JNJ-56021927 Tablet Formulation 1|Drug: JNJ-56021927 Tablet Formulation 2|Drug: JNJ-56021927 Tablet Formulation 3 Aragon Pharmaceuticals, Inc. Phase 1 2014-06-01 2016-10-19
    NCT02903368 Prostate Cancer Drug: Apalutamide|Drug: Leuprolide|Drug: Prednisone|Drug: Abiraterone Acetate|Procedure: Radical Prostatectomy|Other: Observation-Post RP Dana-Farber Cancer Institute|Janssen Scientific Affairs, LLC Phase 2 2016-10-01 2017-02-06
    NCT03088124 Low Risk Prostate Cancer Drug: Apalutamide Institut Paoli-Calmettes|Janssen-Cilag Ltd. Phase 2 2017-03-27 2017-03-17

    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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