EMD 1214063是高活性c-Met选择性抑制剂,IC50为4 nM,比对IRAK4,TrkA,Axl,IRAK1和Mer的抑制性高200倍以上。
Tepotinib (EMD 1214063) is a potent and selective c-Met inhibitor with IC50 of 4 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Phase 1.
15mg/kg每天
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] Bladt F, et al. Clin Cancer Res, 2013, 19(11), 2941-2951.
分子式 C29H28N6O2 |
分子量 492.57 |
CAS号 1100598-32-0 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 5 mg/mL |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT02002650 | Post-ERCP Acute Pancreatitis | Drug: Pre-ERCP rectal Indomethacin|Drug: Post-operational Rectal Indomethacin | Fourth Military Medical University | 2013-12-01 | 2016-05-27 | |
NCT02110810 | Post ERCP Acute Pancreatitis | Drug: Indomethacin|Drug: 2.6-g suppository of glycerin | Instituto Mexicano del Seguro Social | Phase 3 | 2014-01-01 | 2015-03-23 |
NCT02642601 | Difficult Embryo Transfer | Drug: Indomethacin(KAHIRA PHARMA&CHEM,IND,CO.CAIRO-EGYPT) | Cairo University | Phase 2|Phase 3 | 2014-03-01 | 2015-12-24 |
NCT02111707 | Acute Pancreatitis | Drug: Rectal indomethacin 100mg one time before or after ERCP | University of Alberta | Phase 4 | 2014-04-01 | 2016-09-14 |
NCT02633969 | Pain, Postoperative | Drug: Indomethacin Capsules low dose|Drug: Indomethacin Capsules high dose | Iroko Pharmaceuticals, LLC | Phase 2 | 2015-12-01 | 2017-01-27 |
NCT01869361 | Preterm Labor | Drug: Indomethacin|Drug: Placebo | MetroHealth Medical Center | 2016-11-01 | 2016-09-13 | |
NCT02692391 | Acute Pancreatitis | Drug: Indomethacin|Drug: Placebo | University of Pittsburgh | Phase 3 | 2014-07-01 | 2017-02-02 |
NCT02221219 | Intraventricular Hemorrhage|Periventricular Leukomalacia|Brain Injury|Renal Injury | Drug: Indomethacin|Procedure: delay in umbilical cord clamp at birth | John Bauer|University of Kentucky | Phase 1|Phase 2 | 2014-08-01 | 2014-08-19 |
NCT00750581 | Patent Ductus Arteriosus | Drug: Indomethacin | University of Calgary | Phase 2|Phase 3 | 2008-08-01 | 2016-08-17 |
NCT01774604 | Post-ERCP Acute Pancreatitis | Drug: Indomethacin|Drug: Placebo | Dartmouth-Hitchcock Medical Center | Phase 3 | 2013-01-01 | 2016-09-28 |
NCT02935205 | Metastatic Prostate Carcinoma|Recurrent Prostate Carcinoma|Stage IV Prostate Cancer | Drug: Enzalutamide|Drug: Indomethacin | University of California, Davis|National Cancer Institute (NCI) | Phase 1|Phase 2 | 2017-01-01 | 2016-10-13 |
NCT01073670 | Hemorrhage | Drug: Indomethacin|Drug: Acetaminophen & Indomethacin|Drug: Acetaminophen | Queen's University | Phase 4 | 2000-08-01 | 2010-02-22 |
NCT01360034 | Obstetric Labor, Premature | Drug: Nifedipine|Drug: Indomethacin | Saint Thomas Hospital, Panama | Phase 3 | 2015-12-01 | 2015-01-01 |
NCT02711358 | Family Planning | Drug: indomethacin suppositories|Drug: placebo | Assiut University | Phase 4 | 2016-03-01 | 2016-11-28 |
NCT00728117 | Patent Ductus Arteriosus | Other: feeding|Other: fasting | University of California, San Francisco | 2008-07-01 | 2012-11-08 | |
NCT01957215 | Ankle Sprain | Drug: Indomethacin|Drug: Placebo | GlaxoSmithKline|Rundo International Pharmaceutical Research & Development Co.,Ltd. | Phase 4 | 2013-10-01 | 2015-05-21 |
NCT02438371 | Preterm Labor | Drug: Nifedipine|Drug: Indomethacin | The University of Texas Health Science Center, Houston | Phase 4 | 2015-05-01 | 2015-12-03 |
NCT02476279 | Post-ERCP Pancreatitis | Other: Indomethacin 100 mg rectally immediately after ERCP, NO prophylactic pancreatic stent placement|Other: Indomethacin 100 mg rectally immediately after ERCP AND prophylactic pancreatic stent placement | Medical University of South Carolina|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) | Phase 3 | 2015-09-01 | 2016-09-12 |
NCT00009646 | Infant, Very Low Birth Weight|Infant, Premature|Ductus Arteriosus, Patent | Drug: indomethacin|Drug: Indomethacin|Drug: Placebo | NICHD Neonatal Research Network|Medical Research Council of Canada|National Center for Research Resources (NCRR) | Phase 3 | 1993-11-01 | 2015-06-03 |
NCT02116309 | Post-ERCP Acute Pancreatitis | Drug: Rectal Indomethacin|Drug: Epinephrine | Johns Hopkins University|American Society for Gastrointestinal Endoscopy|Asian Institute of Gastroenterology, India|Postgraduate Institute of Medical Education and Research|Apollo Gleneagles Hospitals, Kolkata | 2014-08-01 | 2017-03-01 |
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。
相关化合物库
使用AMQUAR产品发表文献后请联系我们