OTSSP167是一种高效的MELK(母体胚胎亮氨酸拉链激酶)抑制剂,IC50为0.41 nM。
OTSSP167 is a highly potent MELK (maternal embryonic leucine zipper kinase) inhibitor with IC50 of 0.41 nM.
0.005-0.1 μM
1 mg/kg , 5mg/kg ,10 mg/kg, 20 mg/kg 口服处理
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] Chung S, et al. Oncotarget, 2012, 3(12), 1629-1640.
[2] Kuner R, et al. The maternal embryonic leucine zipper kinase (MELK) is upregulated in high-grade prostate cancer. J Mol Med (Berl). 2013 Feb;91(2):237-48. doi: 10.1007/s00109-012-0949-1.
分子式 C25H28Cl2N4O2 |
分子量 487.42 |
CAS号 1431697-89-0 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 0.8 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 |
NCT01245855 | Prostaglandin E1|Percutaneous Coronary Intervention | Drug: lipo-PGE1 | First Affiliated Hospital, Sun Yat-Sen University | Phase 3 | 2011-01-01 | 2010-11-22 |
NCT01776320 | Erectile Dysfunction | Drug: Alprostadil | Lawson Health Research Institute | Phase 4 | 2013-12-01 | 2014-03-03 |
NCT02889822 | Cardiovascular Diseases | Drug: Alprostadil Liposomes for Injection | Guangzhou Yipinhong Pharmaceutical CO.,LTD | Phase 1 | 2010-03-01 | 2016-09-12 |
NCT00619229 | Macular Degeneration | Drug: Alprostadil (prostaglandin E1)|Other: Placebo | UCB Pharma | Phase 3 | 2006-07-01 | 2014-10-17 |
NCT02895373 | Respiratory Distress Syndrome, Adult|Extracorporeal Membrane Oxygenation | Drug: Alprostadil|Drug: 0.9% sodium chloride solution | Thomas Staudinger|Medical University of Vienna | Phase 2 | 2016-07-01 | 2016-09-12 |
NCT00596752 | Peripheral Arterial Occlusive Disease | Drug: Alprostadil|Other: Placebo | UCB BIOSCIENCES GmbH|Aptiv Solutions|UCB Pharma | Phase 4 | 2004-03-01 | 2015-02-26 |
NCT00733434 | Microsurgery|Head and Neck|Prostaglandin E1|Thrombosis|Complications | Drug: Prostaglandin E1|Other: Saline | National Taiwan University Hospital | Phase 4 | 2008-07-01 | 2009-10-26 |
NCT02877173 | Arteriosclerosis Obliterans | Drug: Alprostadil Liposomes for Injection|Drug: Alprostadil Injection | Guangzhou Yipinhong Pharmaceutical CO.,LTD | Phase 2 | 2016-08-01 | 2017-03-08 |
NCT02628106 | Diabetic Nephropathy | Drug: Lipo-PGE1 | West China Hospital | Phase 4 | 2015-12-01 | 2016-11-02 |
NCT00598429 | Infant, Newborn|Respiratory Insufficiency|Pulmonary Hypertension|Respiratory Distress Syndrome, Newborn|Streptococcal Infections | Drug: Inhaled Prostaglandin E1 | NICHD Neonatal Research Network|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) | Phase 2 | 2008-05-01 | 2016-12-08 |
NCT01263925 | Stage II Peripheral Arterial Occlusive Disease|Intermittent Claudication Fontaine Stage II PAOD | Drug: Alprostadil (Prostaglandin E1)|Drug: Pentoxifylline|Drug: Placebo to Pentoxifylline oral|Drug: Placebo to Alprostadil (Prostaglandin E1) intravenous | UCB Pharma | Phase 3 | 2001-04-01 | 2014-10-17 |
NCT00610051 | Heart Failure | Drug: Alprostadil | Biopeutics Co., Ltd | Phase 3 | 2012-12-01 | 2017-01-30 |
NCT01810575 | Erectile Dysfunction | Drug: WC3036-11F/Alprostadil in Vehicle 2.5%|Drug: WC3036-12F/Alprostadil in Vehicle 0.5%|Drug: WC3036-13P/Vehicle Only 0.5% | Warner Chilcott | Phase 2 | 2013-02-01 | 2014-08-08 |
NCT00314548 | Adult Respiratory Distress Syndrome|Pulmonary Hypertension | Drug: PGE1 (prostacyclin)|Drug: normal saline | Aga Khan University|Medical Research Council, Pakistan | 2006-05-01 | 2010-05-18 | |
NCT01467076 | Prematurity|Respiratory Insufficiency|Pulmonary Hypertension|Respiratory Distress Syndrome, Newborn | Drug: Aerosolized Normal Saline|Drug: Inhaled PGE1 | NICHD Neonatal Research Network|National Center for Research Resources (NCRR)|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) | Phase 2 | 2011-11-01 | 2016-11-03 |
NCT02350218 | Evidence of Liver Transplantation | Drug: Eglandin | Asan Medical Center | Phase 2 | 2015-03-01 | 2017-01-23 |
NCT00324948 | Sexual Dysfunction, Physiological | Drug: Topical alprostadil (PGE-1) | VIVUS, Inc. | Phase 2 | 2004-09-01 | 2009-03-09 |
NCT00053716 | Peripheral Vascular Disease | Drug: Liprostin [liposomal Prostaglandin E1] | Endovasc | Phase 2 | 2003-02-01 | 2007-03-06 |
NCT02223949 | Obesity|Labor Complications | Device: Cook double balloon catheter|Drug: PGE1 tablet | Hillel Yaffe Medical Center | Phase 2|Phase 3 | 2014-10-01 | 2014-08-21 |
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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