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Tepotinib

特泊替尼 MSC-2156119,MSC 2156119,MSC2156119,EMD 1214063,EMD-1214063,EMD1214063,

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。

目录号
EY0952
EY0952
EY0952
纯度
99.65%
99.65%
99.65%
规格
5 mg
10 mg
25 mg
原价
1,099_
1,758_
3,080_
售价
1,099_
1,758_
3,080_
库存
预定
预定
预定
订购
订购
订购
订购
订购
订购
  • 生物活性

    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.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

    15mg/kg每天

  • 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] 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

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

    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。

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