LCL161是口服生物相容性的SMAC模拟物,是凋亡蛋白抑制因子抑制剂,具有抗肿瘤活性。
LCL161, a SMAC mimetic, potently binds to and inhibits multiple IAPs (i.e. XIAP, c-IAP). Phase 2.
~10 μM
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] Weisberg E, et al. Leukemia, 2010, 24(12), 2100-2109.
分子式 C26H33FN4O3S |
分子量 500.63 |
CAS号 1005342-46-0 |
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 20 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT01968915 | Neoplasms | Drug: LCL161|Drug: Paclitaxel | Novartis Pharmaceuticals|Novartis | Phase 1 | 2013-11-01 | 2016-01-20 |
NCT01240655 | Solid Tumors | Drug: LCL161|Drug: Paclitaxel | Novartis Pharmaceuticals|Novartis | Phase 1 | 2011-04-01 | 2016-09-01 |
NCT01934634 | Metastatic Pancreatic Cancer | Drug: LCL161|Drug: Gemcitabine|Drug: nab-Paclitaxel | US Oncology Research|Novartis Pharmaceuticals|Delta Clinical Research, LLC | Phase 1 | 2014-03-01 | 2015-11-07 |
NCT01955434 | Recurrent Plasma Cell Myeloma|Refractory Plasma Cell Myeloma | Drug: Cyclophosphamide|Other: Laboratory Biomarker Analysis|Other: Pharmacological Study|Other: Quality-of-Life Assessment|Drug: Smac Mimetic LCL161 | Mayo Clinic|National Cancer Institute (NCI) | Phase 2 | 2013-11-01 | 2017-03-21 |
NCT01098838 | Advanced Solid Tumors | Drug: LCL161 | Novartis Pharmaceuticals|Novartis | Phase 1 | 2008-11-01 | 2012-08-02 |
NCT01617668 | Breast Cancer | Drug: LCL161|Drug: paclitaxel | Novartis Pharmaceuticals|Novartis | Phase 2 | 2012-08-01 | 2016-08-30 |
NCT02649673 | Small Cell Lung Cancer|Ovarian Cancer | Drug: LCL161|Drug: Topotecan | SCRI Development Innovations, LLC|Novartis Pharmaceuticals | Phase 1|Phase 2 | 2016-03-01 | 2016-09-26 |
NCT02098161 | Leukemia | Drug: LCL-161|Behavioral: Questionnaires|Other: Phone Calls | M.D. Anderson Cancer Center|Novartis | Phase 2 | 2014-12-01 | 2016-12-05 |
NCT02890069 | Colorectal Cancer|Non-small Cell Lung Carcinoma (Adenocarcinoma)|Triple Negative Breast Cancer | Biological: PDR001|Drug: LCL161|Drug: Everolimus|Drug: Panobinostat | Novartis Pharmaceuticals|Novartis | Phase 1 | 2016-10-26 | 2017-02-27 |
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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