Hesperadin

Hesperadin是ATP竞争性Aurora B抑制剂,IC50为250 nM。

目录号
EY1547
EY1547
EY1547
EY1547
EY1547
纯度
99.22%
99.22%
99.22%
99.22%
99.22%
规格
1 mg
5 mg
10 mg
50 mg
100 mg
原价
340
780
1420
5230
8800
售价
340
780
1420
5230
8800
库存
现货
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Hesperadin potently inhibits Aurora B with IC50 of 250 nM in a cell-free assay. It markedly reduces the activity of AMPK, Lck, MKK1, MAPKAP-K1, CHK1 and PHK while it does not inhibit MKK1 activity in vivo.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    500 nM 左右

  • 动物实验

  • 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] Hauf S, et al. J Cell Biol, 2003, 161(2), 281-294.

    分子式
    C29H32N4O3S
    分子量
    516.65
    CAS号
    422513-13-1
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    ≥100 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
    NCT02365532 Long QT Syndrome Drug: GS-6615|Drug: Placebo to match GS-6615|Drug: Placebo to match dofetilide|Drug: Dofetilide Gilead Sciences Phase 1 2015-02-01 2015-05-19
    NCT01877486 Paroxysmal Atrial Fibrillation|Persistent Atrial Fibrillation Procedure: Ablation University of Rochester|Medtronic Phase 4 2016-01-01 2016-10-02
    NCT02439658 Long QT Syndrome|Drug Toxicity Drug: Dofetilide and/or sotalol Massachusetts General Hospital|VA Office of Research and Development|Beth Israel Deaconess Medical Center|Brigham and Women's Hospital 2014-01-01 2016-03-27
    NCT02308748 Drug-induced QT Prolongation|Pharmacokinetics|Pharmacodynamics Drug: Dofetilide|Drug: Mexiletine|Drug: Lidocaine|Drug: Moxifloxacin|Drug: Diltiazem|Drug: Placebo Food and Drug Administration (FDA)|Spaulding Clinical Research LLC Phase 1 2014-05-01 2016-06-06
    NCT01873950 Drug-induced Surface ECG Changes Drug: Ranolazine|Drug: Dofetilide|Drug: Verapamil|Drug: Quinidine sulfate|Drug: Placebo Food and Drug Administration (FDA)|Spaulding Clinical Research LLC Phase 1 2013-05-01 2015-12-14
    NCT02241252 Cardiac Arrhythmia|Qt Interval, Variation in Device: iPhone ECG University of Oklahoma 2013-09-01 2015-05-28
    NCT03070470 Drug-induced QT Prolongation|Pharmacokinetics|Pharmacodynamics Drug: Ranolazine|Drug: Verapamil|Drug: Lopinavir / Ritonavir|Drug: Chloroquine|Drug: Placebo|Drug: Dofetilide and Diltiazem Food and Drug Administration (FDA)|Spaulding Clinical Research LLC Phase 1 2017-03-14 2017-03-18
    NCT01505296 Atrial Fibrillation Drug: Antiarrhythmic drug|Procedure: Catheter ablation Valley Health System|Biosense Webster, Inc. Phase 4 2011-12-01 2014-12-13
    NCT00408200 Atrial Fibrillation Drug: propafenone; flecainide; sotalol; dofetilide|Device: Radiofrequency catheter ablation University of Pennsylvania 2006-11-01 2013-01-31
    NCT00540787 Paroxysmal Atrial Fibrillation Device: Radiofrequency ablation, antiarrhythmic drugs|Drug: Amiodarone, flecainide, propafenone, quinidine, dofetilide, sotalol, cibenzoline, beta blocking and calcium channel blocking agents and antiarrhythmic drugs|Device: ThermoCool Radiofrequency Catheter Biosense Webster, Inc. Phase 4 2003-08-01 2012-02-21
    NCT00392106 Atrial Fibrillation Drug: propafenone|Drug: flecainide|Drug: dofetilide|Drug: sotolol|Device: Pulmonary vein ablation|Drug: Amiodarone ProRhythm, Inc. Phase 3 2006-04-01 2008-06-16
    NCT02214069 Atrial Fibrillation|Atrial Flutter Device: Record and transmit heart rhythm The Cleveland Clinic|AliveCor 2014-08-01 2017-01-24
    NCT00589303 Atrial Fibrillation|Heart Failure Drug: FDA approved rate and rhythm control drugs|Device: AV Node ablation and device implant Mayo Clinic|Medtronic Phase 3 2007-12-01 2013-02-25
    NCT01877473 Persistent Atrial Fibrillation Procedure: Ablation Valley Health System Phase 4 2013-05-01 2014-06-16
    NCT01097330 Defibrillators, Implantable|Tachycardia, Ventricular Procedure: Ablation|Drug: Amiodarone Population Health Research Institute|St. Jude Medical|Hamilton Health Sciences Corporation Phase 3 2010-08-01 2011-08-04
    NCT00911508 Atrial Fibrillation|Arrhythmia Device: Left atrial ablation|Drug: Rate or Rhythm Control Therapy Mayo Clinic|National Heart, Lung, and Blood Institute (NHLBI)|St. Jude Medical|Biosense Webster, Inc. 2009-08-01 2016-04-25
    NCT00578617 Atrial Fibrillation|Arrhythmia Drug: Rate Control|Device: Ablation Therapy|Drug: Rate Control|Drug: Rate control|Drug: Rate control|Drug: Rate control|Drug: Rate Control|Drug: Rate Control|Drug: Rate Control|Drug: Rhythm Control|Drug: Rhythm control|Drug: Rhythm control|Drug: Rhythm control|Drug: Rhythm control|Drug: Rhythm control Mayo Clinic|Duke Clinical Research Institute|St. Jude Medical 2006-09-01 2012-12-03

    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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