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。
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.
10 μM
30 mg/kg/天口服
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。
[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
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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