ABT-751(E 7010)是新型的生物相容性的微管蛋白结合剂和抗有丝分裂磺胺类化合物,对神经母细胞瘤细胞株和非神经母细胞瘤细胞株的IC50分别为1.5 和 3.4 μM。
ABT-751 (E7010) binds to the colchicine site on β-tubulin and inhibits polymerization of microtubules, not a substrate for the MDR transporter and is active against cell lines resistant to vincristine, doxorubicin, and cisplatin. Phase 1/2.
0 -100 μM
75 或100 mg/kg/day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] Meany HJ, et al. Pediatr Blood Cancer. 2010, 54(1), 47-54.
[2] Holly J. Meany,et al. Clinical Outcome in Children with Recurrent Neuroblastoma Treated with ABT-751 and Effect of ABT-751 on Proliferation of Neuroblastoma Cell Lines and on Tubulin Polymerization In Vitro. Pediatr Blood Cancer. Author manuscript; available in PMC 2011 Jan 1. Published in final edited form as: Pediatr Blood Cancer. 2010 Jan; 54(1): 47–54. doi: 10.1002/pbc.22267.
[3] Charles M. Rudin,et al. Phase I/II Study of Pemetrexed With or Without ABT-751 in Advanced or Metastatic Non–Small-Cell Lung Cancer. J Clin Oncol. 2011 Mar 10; 29(8): 1075–1082. Published online 2011 Feb 7. doi: 10.1200/JCO.2010.32.5944.
分子式 C18H17N3O4S |
分子量 371.41 |
CAS号 141430-65-1 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO ≥70 mg/mL |
Water <1 mg/mL |
Ethanol ≥10 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT00471718 | Prostate Cancer | Drug: ABT-751 | Vanderbilt-Ingram Cancer Center|National Cancer Institute (NCI) | Phase 1|Phase 2 | 2004-01-01 | 2012-06-27 |
NCT00735878 | Non Small Cell Lung Cancer|Advanced Lung Cancer | Drug: ABT-751 and Carboplatin | Dartmouth-Hitchcock Medical Center|Abbott | Phase 1|Phase 2 | 2004-09-01 | 2009-04-29 |
NCT00436852 | Disseminated Neuroblastoma|Recurrent Neuroblastoma | Drug: ABT-751|Procedure: quality-of-life assessment | Children's Oncology Group|National Cancer Institute (NCI) | Phase 2 | 2007-01-01 | 2017-01-30 |
NCT00047489 | Hematological Malignancies | Drug: ABT-751 | M.D. Anderson Cancer Center | Phase 1 | 2002-12-01 | 2012-02-20 |
NCT00073138 | Colorectal Cancer | Drug: ABT-751 | Abbott | Phase 2 | 2003-08-01 | 2007-11-28 |
NCT00073112 | Renal Cell Cancer | Drug: ABT-751 | Abbott | Phase 2 | 2003-08-01 | 2007-11-28 |
NCT00073151 | Non-Small Cell Lung Cancer | Drug: ABT-751 | Abbott | Phase 2 | 2003-09-01 | 2007-11-28 |
NCT00036959 | Brain and Central Nervous System Tumors|Childhood Germ Cell Tumor|Extragonadal Germ Cell Tumor|Kidney Cancer|Liver Cancer|Neuroblastoma|Ovarian Cancer|Sarcoma|Unspecified Childhood Solid Tumor, Protocol Specific | Drug: ABT-751 | National Institutes of Health Clinical Center (CC)|National Cancer Institute (NCI) | Phase 1 | 2002-03-01 | 2012-03-14 |
NCT00063102 | Breast Cancer | Drug: ABT-751 | Abbott | Phase 2 | 2002-11-01 | 2007-11-28 |
NCT00354562 | Lung Cancer|Non-Small Cell Lung Cancer | Drug: ABT-751|Drug: Placebo|Drug: Docetaxel | Abbott | Phase 1|Phase 2 | 2007-02-01 | 2011-01-05 |
NCT00297089 | Lung Cancer|NSCLC|Non-Small-Cell Lung Cancer | Drug: ABT-751|Drug: pemetrexed|Drug: placebo | AbbVie (prior sponsor, Abbott)|AbbVie | Phase 1|Phase 2 | 2006-11-01 | 2013-01-29 |
NCT00439296 | Recurrent Pediatric ALL|Relapsed Pediatric ALL|Acute Lymphoblastic Leukemia|Refractory Pediatric ALL | Drug: ABT-751|Drug: dexamethasone|Drug: PEG-asparaginase|Drug: doxorubicin|Drug: cytarabine|Drug: methotrexate|Drug: cyclophosphamide|Drug: 6-thioguanine | Therapeutic Advances in Childhood Leukemia Consortium | Phase 1 | 2006-05-01 | 2012-11-28 |
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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