SN-38是CPT-11的一种活性代谢物,抑制DNA topoisomerase I(DNA拓扑异构酶I) ,IC50为1 μM,抑制DNA合成,且造成频繁的DNA单链断裂。
SN-38(NK-012) is an active metabolite of CPT-11, inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks.
0 -1000 nM
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] Kawato Y, et al. Cancer Res, 1991, Aug 15, 51(16), 4187-4191.
[2] Koizumi, F., et al. 2006. Cancer Res. 66: 10048-10056.
[3] Gao, H., et al. 2005. Bioorg. Med. Chem. Lett. 15: 3233-3236.
分子式 C22H20N2O5 |
分子量 392.4 |
CAS号 86639-52-3 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 25 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 |
NCT00311610 | Colorectal Cancer | Drug: SN-38 liposome | Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI) | Phase 2 | 2006-01-01 | 2016-06-28 |
NCT00104754 | Lung Cancer | Drug: liposomal SN-38 | Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI) | Phase 2 | null | 2016-07-19 |
NCT00734682 | Glioblastoma|Gliosarcoma|Anaplastic Astrocytoma|Anaplastic Oligodendroglioma | Drug: Nanoliposomal CPT-11 | University of California, San Francisco | Phase 1 | 2008-08-01 | 2015-01-05 |
NCT00509860 | Sarcoma | Drug: Irinotecan | M.D. Anderson Cancer Center | Phase 2 | 2003-03-01 | 2012-12-28 |
NCT02171325 | Small Cell Lung Cancer | Drug: irinotecan | Guangdong Association of Clinical Trials | Phase 2 | 2014-06-01 | 2014-06-20 |
NCT00644696 | Neuroblastoma | Drug: Irinotecan and Bortezomib | University of Michigan Cancer Center|Millennium Pharmaceuticals, Inc. | Phase 1 | 2008-04-01 | 2016-06-02 |
NCT01607554 | Non-small Cell Lung Cancer | Drug: Irinotecan | New Mexico Cancer Care Alliance|University of New Mexico Cancer Center|Lovelace Respiratory Research Institute | Phase 1|Phase 2 | 2012-04-01 | 2016-06-07 |
NCT00969033 | Metastatic Colorectal Cancer | Drug: CS-1008|Drug: irinotecan | Daiichi Sankyo Inc. | Phase 2 | 2009-07-01 | 2012-01-30 |
NCT00353015 | Gastrointestinal Cancer|Carcinoma, Neuroendocrine | Drug: Cisplatin|Drug: Irinotecan | M.D. Anderson Cancer Center|Pharmacia | Phase 2 | 2003-03-01 | 2012-08-01 |
NCT00808184 | Solid Tumor | Drug: CPT-11, Raltegravir (Isentress庐), Midazolam | National University Hospital, Singapore | Phase 4 | 2010-04-01 | 2012-10-31 |
NCT00003748 | Esophageal Cancer|Gastric Cancer | Drug: irinotecan hydrochloride | Jonsson Comprehensive Cancer Center|National Cancer Institute (NCI)|Pharmacia and Upjohn | Phase 2 | 1998-08-01 | 2015-10-28 |
NCT01654081 | Lung Cancer | Drug: Irinotecan | Susanne Arnold|University of Kentucky | Phase 2 | 2013-10-01 | 2014-05-28 |
NCT01114555 | Neuroblastoma | Drug: Bevacizumab, Irinotecan and Temozolomide | Memorial Sloan Kettering Cancer Center|Genentech, Inc. | Phase 2 | 2010-04-01 | 2016-05-09 |
NCT01016860 | Colorectal Cancer | Drug: OSI-906|Drug: irinotecan | University of Colorado, Denver | Phase 1 | 2009-12-01 | 2013-10-18 |
NCT00563316 | Metastatic Colorectal Cancer | Drug: Panitumumab|Drug: Irinotecan | Amgen | Phase 1 | 2008-03-01 | 2016-03-14 |
NCT01036113 | Metastatic Breast Cancer | Drug: EZN-2208 | Enzon Pharmaceuticals, Inc. | Phase 2 | 2009-11-01 | 2012-10-01 |
NCT00532714 | Breast Cancer Metastatic | Drug: Irinotecan plus capecitabine | National Cancer Center, Korea | Phase 2 | 2006-08-01 | 2011-12-27 |
NCT03053167 | ColoRectal Cancer | Drug: Irinotecan|Drug: Raltitrexed | China Medical University, China|The First Affiliated Hospital of Dalian Medical University|The Second Affiliated Hospital of Dalian Medical University|Liaoning Tumor Hospital & Institute|Shengjing Hospital|General Hospital of Shenyang Military Region | Phase 2 | 2016-12-01 | 2017-02-13 |
NCT01847495 | Colorectal Cancer | Drug: Irinotecan|Radiation: CyberKnife | Advocate Health Care | 2013-10-01 | 2017-01-26 | |
NCT01826396 | Colonic Neoplasms | Drug: Irinotecan | Colorectal Cancer Institute of the Heilongjiang Academy of Medical Sciences | Phase 2 | 2013-04-01 | 2013-04-04 |
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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