LDE225 (NVP-LDE225,Erismodegib)是一种Smoothened(Smo)拮抗剂,抑制Hedgehog (Hh)信号通路,IC50分别为1.3 nM (小鼠)和2.5 nM(人)。
LDE225(synonym: LDE-225, NVP-LDE225, Erismodegib) is a Smoothened (Smo) antagonist, inhibiting Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human), respectively.
0.5% CMC
0 μM -10 μM
40 mg/kg/天口服,每天两次
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] Pan SF, et al. ACS Med. Chem. Lett., 2010, 1 (3), 130–134.
分子式 C26H26F3N3O3 |
分子量 485.5 |
CAS号 956697-53-3 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO >90 mg/mL |
Water <1 mg/mL |
Ethanol >90 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT02111187 | Prostate Cancer | Drug: LDE225 | Sidney Kimmel Comprehensive Cancer Center | Phase 1 | 2014-04-01 | 2016-10-14 |
NCT02195973 | Recurrent Ovarian Cancer | Drug: LDE225 | University of Alabama at Birmingham|Novartis Pharmaceuticals | Phase 1 | 2014-09-01 | 2017-02-06 |
NCT01764776 | Normal Hepatic Function|Impaired Hepatic Function | Drug: LDE225 | Novartis Pharmaceuticals|Novartis | Phase 1 | 2013-03-01 | 2017-02-13 |
NCT02086513 | Graft Versus Host Disease | Drug: LDE225 | Massachusetts General Hospital|Novartis | Phase 1 | 2014-04-01 | 2017-03-21 |
NCT02254551 | Multiple Myeloma | Drug: LDE225|Drug: Bortezomib | SCRI Development Innovations, LLC|Novartis | Phase 2 | 2015-01-01 | 2016-12-23 |
NCT01529450 | Basal Cell Carcinoma | Drug: LDE225 | Anne Chang|Novartis|Stanford University | 2012-02-01 | 2016-11-23 | |
NCT02002689 | PTCH1 or SMO Activated Solid and Hematologic Tumors | Drug: LDE225 | Novartis Pharmaceuticals|Novartis | Phase 2 | 2014-02-01 | 2016-04-25 |
NCT01954355 | Solid Tumor|Ovarian Cancer | Drug: LDE225|Drug: Paclitaxel | Swiss Group for Clinical Cancer Research | Phase 1 | 2013-09-01 | 2016-11-23 |
NCT01208831 | Advanced Solid Tumor Cancers|Medulloblastoma|Basal Cell Carcinoma | Drug: LDE225 | Novartis Pharmaceuticals|Novartis | Phase 1 | 2010-10-01 | 2016-04-20 |
NCT00880308 | Advanced Solid Tumor Cancers|Medulloblastoma|Basal Cell Carcinoma | Drug: LDE225 | Novartis Pharmaceuticals|Novartis | Phase 1 | 2009-03-01 | 2014-12-27 |
NCT02151864 | Hepatocellular Carcinoma|Cirrhosis | Drug: LDE225 | Jason K. Sicklick, M.D.|Novartis Pharmaceuticals|University of California, San Diego | Phase 1 | 2014-07-01 | 2016-09-27 |
NCT01487785 | Pancreatic Cancer | Drug: LDE225+gemcitabine | Novartis Pharmaceuticals|Novartis | Phase 1 | 2012-03-01 | 2016-01-24 |
NCT01826214 | Acute Leukemias | Drug: LDE225 | Novartis Pharmaceuticals|Novartis | Phase 2 | 2013-05-01 | 2016-07-26 |
NCT02027376 | Advanced Breast Cancer | Drug: LDE225|Drug: Docetaxel | Spanish Breast Cancer Research Group|Novartis | Phase 1 | 2014-05-01 | 2015-11-05 |
NCT01125800 | Medulloblastoma|Rhabdomyosarcoma|Neuroblastoma|Hepatoblastoma|Glioma|Astrocytoma | Drug: LDE225 | Novartis Pharmaceuticals|Novartis | Phase 1|Phase 2 | 2011-02-01 | 2017-02-13 |
NCT01579929 | Lung Cancer | Drug: LDE225, Etoposide and Cisplatin | Memorial Sloan Kettering Cancer Center|Novartis Pharmaceuticals | Phase 1 | 2012-04-01 | 2017-02-15 |
NCT01694589 | Resectable Pancreatic Cancer | Drug: LDE-225 | Rutgers, The State University of New Jersey|Rutgers Cancer Institute of New Jersey|National Cancer Institute (NCI)|Novartis Pharmaceuticals | Early Phase 1 | 2012-11-01 | 2014-12-10 |
NCT02138929 | Esophageal Cancer | Drug: Everolimus|Drug: LDE 225 | M.D. Anderson Cancer Center|Novartis|National Cancer Institute (NCI) | Phase 1 | 2014-11-01 | 2016-09-30 |
NCT01456676 | Philadelphia Chromosome Positive Chronic Myelogenous Leukemia | Drug: Nilotinib + LDE225 | Novartis Pharmaceuticals|Novartis | Phase 1 | 2012-01-01 | 2016-09-01 |
NCT01327053 | Basal Cell Carcinoma | Drug: LDE225 | Novartis Pharmaceuticals|Novartis | Phase 2 | 2011-06-01 | 2016-09-20 |
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