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/ 微管 / Fosbretabulin disodium

康普瑞汀磷酸二钠 /Fosbretabulin disodium {[allProObj[0].p_purity_real_show]}

货号：A116116 同义名： 康普瑞汀A4磷酸二钠 / Combretastatin A4 disodium phosphate;CA 4P

Fosbretabulin disodium是Combretastatin A4（CA4）的水溶性前药，CA4是一种微管靶向药物，可以与β-微管蛋白结合，Kd为0.4 μM（在无细胞实验中）。Fosbretabulin disodium能够抑制微管蛋白的聚合，IC50为2.4 μM，并且破坏肿瘤血管。

Fosbretabulin disodium 化学结构 CAS号：168555-66-6
Fosbretabulin disodium 化学结构
CAS号：168555-66-6
Fosbretabulin disodium 3D分子结构
CAS号：168555-66-6
Fosbretabulin disodium 化学结构 CAS号：168555-66-6
Fosbretabulin disodium 3D分子结构 CAS号：168555-66-6
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Fosbretabulin disodium 纯度/质量文件 产品仅供科研

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Fosbretabulin disodium 生物活性

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].
体内研究

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].
体外研究

Fosbretabulin disodium effectively inhibits the growth of various cancer cell lines including leukemia P-388, pancreas BXPC-3, neuroblastoma SK-N-SH, thyroid SW1736, lung-NSC NCI-H460, prostate DU-145, and pharynx FADU, displaying EC50 values ranging from 0.00025 to 0.23 μg/mL[2].

Fosbretabulin disodium 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 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

Fosbretabulin disodium 动物研究

Dose Mice: 150 mg/kg[3] (i.p.) Rat: 3 mg/kg[4] (i.p.),
Administration i.p.

Fosbretabulin disodium 临床研究

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 <<

Fosbretabulin disodium 参考文献

[1]Shen CH, et, al. Combretastatin A-4 inhibits cell growth and metastasis in bladder cancer cells and retards tumour growth in a murine orthotopic bladder tumour model. Br J Pharmacol. 2010 Aug;160(8):2008-27.

[2]Pettit GR, et, al. Antineoplastic agents. 445. Synthesis and evaluation of structural modifications of (Z)- and (E)-combretastatin A-41. J Med Chem. 2005 Jun 16;48(12):4087-99.

[3]Tozer GM, et, al. Combretastatin A-4 phosphate as a tumor vascular-targeting agent: early effects in tumors and normal tissues. Cancer Res. 1999 Apr 1;59(7):1626-34.

Fosbretabulin disodium 实验方案

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

Fosbretabulin disodium 技术信息

CAS号168555-66-6
分子式C18H19Na2O8P
分子量 440.292
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
溶解度

H2O: 4 mg/mL(9.08 mM)
动物实验配方

Tags: Fosbretabulin disodium | 168555-66-6 | CA 4DP | CA 4P | Combretastatin A4 disodium | Cell Cycle/DNA Damage | Cytoskeleton | Apoptosis | Microtubule/Tubulin | Apoptosis | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Fosbretabulin disodium 纯度/质量文件 | Fosbretabulin disodium 生物活性 | Fosbretabulin disodium 细胞研究 | Fosbretabulin disodium 动物研究 | Fosbretabulin disodium 临床数据 | Fosbretabulin disodium 参考文献 | Fosbretabulin disodium 实验方案 | Fosbretabulin disodium 技术信息

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