货号:A116116
同义名:
康普瑞汀A4磷酸二钠
/ Combretastatin A4 disodium phosphate; CA 4P
Fosbretabulin disodium is the water-soluble prodrug of Combretastatin A4 (CA4), which is a microtubule-targeting agent that binds β-tubulin with Kd of 0.4 μM in a cell-free assay. Fosbretabulin disodium inhibits the polymerization of tubulin with IC50 of 2.4 μM, and also disrupts tumor vasculature.
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描述 | Fosbretabulin disodium (CA 4DP) is a tubulin destabilizing agent and is a proagent of Combretastatin A4, specifically targeting endothelial cells. It induces the regression of nascent tumor neovessels, diminishes tumor blood flow, and leads to central tumor necrosis[1].[3]. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活性说明 | 数据源 |
HeLa cells | Proliferation assay | Antiproliferative activity against human HeLa cells by sulforhodamine B assay, IC50=0.0047 μM | 20973488 | ||
rat A10 cells | Function assay | Inhibition of microtubule depolymerization in rat A10 cells assessed as reorganization of interphase microtubule network by indirect immunofluorescence technique, EC50=0.007 μM | 20973488 | ||
SKOV3 cells | Proliferation assay | Antiproliferative activity against human SKOV3 cells by sulforhodamine B assay, IC50=0.0045 μM | 20973488 |
Animal study | Additionally, administration of Fosbretabulin disodium (100 mg/kg; intraperitoneally) has been shown to increase the mean arterial blood pressure (MABP) 1 and 6 hours post-administration and reduce tumor blood flow in rats[3]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT00507429 | Anaplastic Thyroid Cancer | Phase 2 Phase 3 | Terminated(Low rate of subject... 展开 >> accrual) 收起 << | - | - |
NCT00395434 | Tumors | Phase 1 | Completed | - | United Kingdom ... 展开 >> Mount Vernon Hospital Northwood, Middlesex, United Kingdom, HA6 2RN Royal Marsden Hospital Sutton, Surrey, United Kingdom, SM2 5PT 收起 << |
NCT00653939 | Tumors | Phase 2 | Completed | - | United States, California ... 展开 >> Southbay Oncology Hematology Campbell, California, United States, 95008 Pacific Coast Hematology and Oncology Medical Group Fountain Valley, California, United States, 92708 UCLA Division of Hematology and Oncology Los Angeles, California, United States, 90095 Bay Area Cancer Research Group, LLC Pleasant Hill, California, United States, 94523 United States, Florida Boca Raton Comprehensive Cancer Center Boca Raton, Florida, United States, 21020 United States, Kentucky Kentuckiana Cancer Institute Louisville, Kentucky, United States, 40202 United States, Massachusetts Lahey Clinic Medical Center Burlington, Massachusetts, United States, 01805 United States, New Jersey The Center for Cancer and Hematologic Disease Cherry Hill, New Jersey, United States, 08003 United States, New Mexico San Juan Oncology Associates Farmington, New Mexico, United States, 87401 United States, Ohio Gabrail Cancer Center Canton, Ohio, United States, 44718 The Mark H. Zangmeister Center Columbus, Ohio, United States, 43219 Signal Point Clinical Research Middletown, Ohio, United States, 45042 United States, Virginia Blueridge Cancer Care Salem, Virginia, United States, 24153 United States, Washington Northwest Medical Specialties Tacoma, Washington, United States, 98405 United States, West Virginia Mary Babb Randolph Cancer Center-Clinical Trials Unit Morgantown, West Virginia, United States, 26506 收起 << |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.27mL 0.45mL 0.23mL |
11.36mL 2.27mL 1.14mL |
22.71mL 4.54mL 2.27mL |
CAS号 | 168555-66-6 |
分子式 | C18H19Na2O8P |
分子量 | 440.29 |
SMILES Code | O=P([O-])([O-])OC1=CC(/C=C\C2=CC(OC)=C(OC)C(OC)=C2)=CC=C1OC.[Na+].[Na+] |
MDL No. | MFCD00943911 |
别名 | 康普瑞汀A4磷酸二钠 ;Combretastatin A4 disodium phosphate; CA 4P; CRC 87-09; Combrestatin A4; Combrestatin A4 3'-O-Phosphate (sodium salt); CA 4DP |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Inert atmosphere, store in freezer, under -20°C |
溶解方案 |
配制的工作液建议现用现配,短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。
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