Alectinib (CH5424802)是一种有效的ALK抑制剂,IC50为1.9 nM,对L1196M突变型敏感,作用于ALK比PF-02341066, NVP-TAE684和PHA-E429选择性高。
Alectinib is a highly selective, orally active and potent ALK inhibitor with IC50 of 1.9 nM.
30% PEG400+0.5% Tween80+5% propylene glycol
0-1 μM
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] Sakamoto H, et al. Cancer Cell. 2011, 19(5), 679-690.
分子式 C30H34N4O2 |
分子量 482.62 |
CAS号 1256580-46-7 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 0.5 mg/mL with gentle warming |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT02521051 | Non-Small Cell Lung Cancer (NSCLC) | Drug: Alectinib|Drug: Bevacizumab | Massachusetts General Hospital|Genentech, Inc. | Phase 1|Phase 2 | 2015-10-01 | 2016-09-12 |
NCT02075840 | Non-Small Cell Lung Cancer | Drug: Alectinib|Drug: Crizotinib | Hoffmann-La Roche | Phase 3 | 2014-08-01 | 2017-02-23 |
NCT02838420 | Anaplastic Lymphoma Kinase-positive Non-small Cell Lung Cancer | Drug: Alectinib|Drug: Crizotinib | Hoffmann-La Roche | Phase 3 | 2016-08-01 | 2016-11-01 |
NCT02621047 | Hepatic Impairment | Drug: Alectinib | Hoffmann-La Roche | Phase 1 | 2015-12-01 | 2017-02-21 |
NCT01984229 | Healthy Volunteer | Drug: Alectinib|Drug: Posaconazole | Hoffmann-La Roche | Phase 1 | 2013-12-01 | 2016-08-16 |
NCT02023125 | Healthy Volunteer | Drug: Alectinib|Drug: Esomeprazole|Other: High Fat and Calorie Meal|Other: Standard Meal | Hoffmann-La Roche | Phase 1 | 2013-12-01 | 2016-08-16 |
NCT02604342 | Non-small Cell Lung Cancer | Drug: Alectinib|Drug: Docetaxel|Drug: Pemetrexed | Hoffmann-La Roche | Phase 3 | 2015-11-03 | 2017-03-14 |
NCT02271139 | Non-Small Cell Lung Cancer | Drug: Alectinib | Genentech, Inc. | null | 2017-03-07 | |
NCT02013219 | Non-Small Cell Lung Cancer | Drug: Alectinib|Drug: Atezolizumab [TECENTRIQ]|Drug: Erlotinib | Hoffmann-La Roche | Phase 1 | 2014-04-03 | 2017-03-17 |
NCT01871805 | Non-Small Cell Lung Cancer | Drug: RO5424802|Drug: RO5424802 | Hoffmann-La Roche | Phase 2 | 2013-09-01 | 2016-07-01 |
NCT01981005 | Healthy Volunteer | Drug: RO5424802 | Hoffmann-La Roche | Phase 1 | 2013-11-01 | 2016-11-01 |
NCT01940510 | Healthy Volunteer | Drug: RO5424802|Drug: rifampin | Hoffmann-La Roche | Phase 1 | 2013-10-01 | 2016-11-01 |
NCT02074553 | Healthy Volunteer | Drug: Part 1 (Fasted): Treatment A|Drug: Part 1 (Fasted): Treatment B|Drug: Part 1 (Fasted): Treatment C|Drug: Part 1 (Fasted): Treatment D|Drug: Part 2 (Fed): Treatment A|Drug: Part 2 (Fed): Treatment B|Drug: Part 2 (Fed): Treatment C|Drug: Part 2 (Fed): Treatment D | Hoffmann-La Roche | Phase 1 | 2014-02-01 | 2016-08-25 |
NCT01588028 | ALK-Rearranged Non-Small Cell Lung Cancer | Drug: CH5424802 | Hoffmann-La Roche | Phase 1 | 2012-04-01 | 2014-10-16 |
NCT01801111 | Non-Squamous Non-Small Cell Lung Cancer | Drug: erlotinib [Tarceva]|Drug: RO5452802 | Hoffmann-La Roche | Phase 2 | 2013-06-01 | 2016-04-11 |
NCT02450903 | Non-Small-Cell Lung Cancer | Drug: LDK378 | Novartis Pharmaceuticals|Novartis | Phase 2 | 2015-08-01 | 2017-02-05 |
NCT02314481 | Non-small Cell Lung Cancer | Drug: MPDL3280A|Drug: Vemurafenib|Drug: Alectinib|Drug: Trastuzumab emtansine | University College, London|Hoffmann-La Roche | Phase 2 | 2017-01-01 | 2016-03-08 |
NCT02706626 | Non-Small Cell Lung Cancer | Drug: brigatinib | Criterium, Inc.|University of Colorado, Denver|Duke University|Ariad Pharmaceuticals | Phase 2 | 2017-03-09 | 2017-03-10 |
NCT03087448 | Non-small Cell Lung Cancer | Drug: Ceritinib|Drug: Trametinib | University of California, San Francisco|Novartis Pharmaceuticals|University of California, Davis|University of California, Los Angeles|University of California, San Diego|University of California, Irvine | Phase 1|Phase 2 | 2017-03-01 | 2017-03-16 |
NCT01634763 | Tumors Characterized by Genetic Alterations in Anaplastic Lymphoma Kinase (ALK) | Drug: LDK378 | Novartis Pharmaceuticals|Novartis | Phase 1 | 2012-06-01 | 2016-07-25 |
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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