Motesanib Diphosphate (AMG-706)是一种有效的ATP竞争性的VEGFR1/2/3抑制剂,IC50分别为2 nM/3 nM/6 nM;对Kit具有相似的抑制活性,对VEGFR选择性比PDGFR和Ret高10倍。
Motesanib Diphosphate (AMG-706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively; similar activity against Kit, ~10-fold more selective for VEGFR than PDGFR and Ret. Phase 3.
~25 μM
~100 mg/kg 口服处理,每天一次或两次
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] Polverino A, et al. Cancer Res, 2006, 66(17), 8715-8721.
分子式 C22H29N5O9P2 |
分子量 569.44 |
CAS号 857876-30-3 |
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 100 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT00427349 | Gastrointestinal Carcinoid Tumor|Islet Cell Tumor|Neoplastic Syndrome | Drug: AMG 706|Drug: octreotide | Eastern Cooperative Oncology Group|National Cancer Institute (NCI) | Phase 2 | 2008-09-01 | 2016-07-12 |
NCT01836549 | Anaplastic Astrocytoma|Anaplastic Ependymoma|Astrocytoma, Grade II|Ependymoma|Giant Cell Glioblastoma|Glioblastoma|Gliosarcoma|Oligodendroglioma|Brainstem Tumors | Drug: imetelstat sodium | Pediatric Brain Tumor Consortium|National Cancer Institute (NCI) | Phase 2 | 2013-03-01 | 2016-04-08 |
NCT00360867 | Solid Tumors | Drug: AMG 706 | Amgen | Phase 2 | 2005-12-01 | 2015-09-24 |
NCT01731951 | Primary Myelofibrosis|Secondary Myelofibrosis|Myeloid Malignancies | Drug: Imetelstat | Janssen Research & Development, LLC | Phase 2 | 2012-10-01 | 2016-12-02 |
NCT01242930 | Multiple Myeloma | Drug: Imetelstat (7.5 mg/kg)|Drug: lenalidomide standard of care|Drug: Imetelstat (9.4 mg/kg) | Geron Corporation | Phase 2 | 2010-11-01 | 2016-04-13 |
NCT00574951 | Fallopian Tube Cancer|Ovarian Cancer|Primary Peritoneal Cavity Cancer | Drug: motesanib diphosphate | Gynecologic Oncology Group|National Cancer Institute (NCI) | Phase 2 | 2007-12-01 | 2015-05-29 |
NCT02011126 | Childhood Hepatoblastoma|Previously Treated Childhood Rhabdomyosarcoma|Recurrent Childhood Liver Cancer|Recurrent Childhood Rhabdomyosarcoma|Recurrent Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor|Recurrent Neuroblastoma|Recurrent Osteosarcoma | Drug: imetelstat sodium|Other: laboratory biomarker analysis | Children's Oncology Group|National Cancer Institute (NCI) | Phase 2 | 2014-06-01 | 2017-02-08 |
NCT01386866 | Advanced Solid Tumors | Drug: AMG 706 | Amgen | Phase 1 | 2009-05-01 | 2011-07-14 |
NCT02426086 | Primary Myelofibrosis | Drug: Imetelstat 9.4 milligram/kilogram (mg/kg)|Drug: Imetelstat 4.7 mg/kg | Janssen Research & Development, LLC | Phase 2 | 2015-06-01 | 2016-10-31 |
NCT01916187 | Neuroblastoma | Drug: Imetelstat | NCIC Clinical Trials Group|Geron Corporation|Canadian Cancer Trials Group | Phase 1 | 2013-07-01 | 2014-02-07 |
NCT01137968 | Non-small Cell Lung Cancer | Drug: imetelstat|Drug: Bevacizumab | Geron Corporation | Phase 2 | 2010-05-01 | 2015-12-22 |
NCT02598661 | Myelodysplastic Syndromes | Drug: Imetelstat|Drug: Placebo | Janssen Research & Development, LLC | Phase 3 | 2015-11-01 | 2017-01-13 |
NCT00254267 | Advanced Gastrointestinal Stromal Tumor | Drug: AMG 706 | Amgen|Takeda Bio Development Center, Ltd | Phase 2 | 2005-11-01 | 2014-02-26 |
NCT02629848 | Carcinoma, Non-Small-Cell Lung | Drug: Motesanib|Drug: Placebo|Drug: Paclitaxel|Drug: Carboplatin | Takeda | Phase 3 | 2012-07-01 | 2015-12-10 |
NCT00356681 | Breast Neoplasms|Breast Tumors|Breast Cancer|Locally Recurrent and Metastatic Breast Cancer | Drug: AMG 706 placebo|Drug: Bevacizumab|Drug: AMG 706|Drug: Paclitaxel | Amgen | Phase 2 | 2006-12-01 | 2015-09-24 |
NCT00094835 | Lung Cancer|Non-Small Cell Lung Cancer | Biological: Panitumumab|Drug: Motesanib diphosphate|Drug: Paclitaxel|Drug: Carboplatin | Amgen | Phase 1|Phase 2 | 2005-01-01 | 2016-02-26 |
NCT00369070 | Advanced Non-squamous NSCLC | Biological: Bevacizumab|Drug: AMG 706|Drug: Paclitaxel|Drug: Carboplatin | Amgen | Phase 2 | 2007-01-01 | 2016-06-09 |
NCT00124189 | Chronic Lymphoproliferative Diseases | Drug: GRN163L | Geron Corporation | Phase 1 | 2005-07-01 | 2015-12-22 |
NCT00093873 | Tumors | Drug: Anti-angiogenesis|Drug: AMG 706 | Amgen | Phase 1 | 2003-07-01 | 2013-05-13 |
NCT01256762 | Locally Recurrent or Metastatic Breast Cancer | Drug: Imetelstat sodium|Drug: Bevacizumab|Drug: Paclitaxel | Geron Corporation | Phase 2 | 2010-11-01 | 2015-12-22 |
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。
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