OSI-420 (Desmethyl Erlotinib,CP-473420)是erlotinib的活性代谢物,是口服活性的EGFR抑制剂,对人EGFR和EGFR自磷酸化的IC50分别为2和20 nM。
OSI-420 is the active metabolite of Erlotinib (EGFR inhibitor with IC50 of 2 nM).
30 nM-20 μM
50 mg/kg口服给药
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] Meany HJ, et al. Cancer Chemother Pharmacol. 2008, 62(3), 387-392.
分子式 C21H22ClN3O4 |
分子量 415.87 |
CAS号 183320-51-6 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 83 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 |
NCT02904850 | Lung Cancer | Biological: group of patients | University Hospital, Strasbourg, France | 2014-06-01 | 2016-09-13 | |
NCT00482625 | Intraductal Papillary Mucinous Neoplasm of the Pancreas|Recurrent Pancreatic Cancer|Stage IA Pancreatic Cancer|Stage IB Pancreatic Cancer|Stage IIA Pancreatic Cancer|Stage IIB Pancreatic Cancer|Stage III Pancreatic Cancer | Drug: erlotinib hydrochloride|Procedure: conventional surgery|Other: immunohistochemistry staining method|Genetic: protein expression analysis|Procedure: biopsy|Other: pharmacological study|Other: laboratory biomarker analysis | National Cancer Institute (NCI) | Phase 2 | 2007-06-01 | 2014-10-07 |
NCT00925769 | Pancreatic Cancer | Drug: bevacizumab [Avastin]|Drug: capecitabine [Xeloda]|Drug: erlotinib [Tarceva] | Hoffmann-La Roche | Phase 1 | 2009-01-01 | 2015-07-13 |
NCT00124657 | Brain and Central Nervous System Tumors | Drug: Erlotinib hydrochloride | St. Jude Children's Research Hospital|Rady Children's Hospital, San Diego|Duke University | Phase 1|Phase 2 | 2005-03-01 | 2015-10-29 |
NCT00754494 | Adenomatous Polyp|Recurrent Colon Cancer|Recurrent Rectal Cancer|Stage I Colon Cancer|Stage I Rectal Cancer|Stage IIA Colon Cancer|Stage IIA Rectal Cancer|Stage IIB Colon Cancer|Stage IIB Rectal Cancer|Stage IIC Colon Cancer|Stage IIC Rectal Cancer|Stage IIIA Colon Cancer|Stage IIIA Rectal Cancer|Stage IIIB Colon Cancer|Stage IIIB Rectal Cancer|Stage IIIC Colon Cancer|Stage IIIC Rectal Cancer | Drug: erlotinib hydrochloride|Other: placebo|Other: laboratory biomarker analysis | National Cancer Institute (NCI) | Phase 2 | 2008-07-01 | 2014-12-22 |
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