Ostarine是选择性雄激素受体调节剂,ED50为0.44 mg/day。
MK-2866 (GTx-024) is a selective androgen receptor modulator (SARM) with Ki of 3.8 nM, and is tissue-selective for anabolic organs. Phase 3.
1 mg/day皮下注射
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] Kim J, et al. J Pharmacol Exp Ther, 2005, 315(1), 230-239.
分子式 C19H14F3N3O3 |
分子量 389.33 |
CAS号 841205-47-8 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 76 mg/mL |
Water <1 mg/mL |
Ethanol 76 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT02658448 | Stress Urinary Incontinence | Drug: GTx-024 | GTx | Phase 2 | 2016-01-01 | 2017-03-14 |
NCT02746328 | ER+ and AR+ Breast Cancer | Drug: GTx-024 9 or 18 mg | GTx | Phase 2 | 2016-04-01 | 2017-03-14 |
NCT02368691 | Triple Negative Breast Cancer | Drug: GTx-024 | GTx | Phase 2 | 2015-06-01 | 2016-08-30 |
NCT01616758 | Metastatic Breast Cancer | Drug: GTx-024 9mg | GTx | Phase 2 | 2013-04-01 | 2017-03-14 |
NCT00467844 | Cachexia | Drug: GTx-024|Drug: GTx-024|Drug: Placebo | GTx | Phase 2 | 2007-05-01 | 2014-06-26 |
NCT02971761 | Androgen Receptor Positive|Estrogen Receptor Negative|HER2/Neu Negative|Progesterone Receptor Negative|Recurrent Breast Carcinoma|Stage III Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer|Triple-Negative Breast Carcinoma | Drug: Enobosarm|Other: Laboratory Biomarker Analysis|Biological: Pembrolizumab | City of Hope Medical Center|National Cancer Institute (NCI) | Phase 2 | 2017-01-01 | 2016-11-21 |
NCT02463032 | ER+ and AR+ Breast Cancer | Drug: GTx-024 | GTx | Phase 2 | 2015-08-01 | 2016-08-31 |
NCT01355497 | Muscle Wasting|Non-Small Cell Lung Cancer | Drug: GTx-024|Drug: placebo | GTx | Phase 3 | 2011-07-01 | 2015-03-18 |
NCT01355484 | Muscle Wasting|Non Small Cell Lung Cancer | Drug: GTx-024|Drug: placebo | GTx | Phase 3 | 2011-07-01 | 2016-02-04 |
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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