Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium
(Synonyms: CA 4DP; CA 4P; Combretastatin A4 disodium phosphate) 目录号 : GC12308
A potent inhibitor of tubulin polymerization
Cas No.:168555-66-6
Sample solution is provided at 25 µL, 10mM.
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Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium is a microtubule destabilizing drug, a water-soluble prodrug of combretasain A4(CA4) and a tumor vascular-targeting agent.
Microtubule is the cylindrical and filamentous structure that required for cell shape, migration, cilia and flagella mobility etc. Tubulin is the major component of microtubules
In proliferative endothelial cells, CA4P (dose less than 1/10 of the max. tolerated dose) leaded to tumor vascular shutdown, and short drug exposure of CA4P caused significant long-term anti-proliferative and cytotoxic effects. [1] In CA40 treated endothelia cell, myosin light chain was phosphorylated and lead to actinomyosin contractility, assembly of actin stress fibers and focal adhesions formation. [2] In HUVEC cells, CA4P blocked growth factor–induced endothelial cell proliferation and migration and impaired capillary tube formation. [3]
In C57BL/6 mice, CA4P treatment in combination with mAb against VE-cardherin facilitated B16 melanoma tumor necrosis and inhibited tumor neoangionesis. [3] In human breast cancer models in vivo, 6 hours after CA4P administration showed a 93% decreased functional vascular volume and lasted over the next 12 hours. [1]
References:
[1] Dark GG, Hill SA, Prise VE, Tozer GM, Pettit GR, Chaplin DJ. Combretastatin A-4, an agent that displays potent and selective toxicity toward tumor vasculature. Cancer Res. 1997 May 15;57(10):1829-34.
[2] Kanthou C, Tozer GM. The tumor vascular targeting agent combretastatin A-4-phosphate induces reorganization of the actin cytoskeleton and early membrane blebbing in human endothelial cells. Blood. 2002 Mar 15;99(6):2060-9.
[3] Vincent L, Kermani P, Young LM, Cheng J, Zhang F, Shido K, Lam G, Bompais-Vincent H, Zhu Z, Hicklin DJ, Bohlen P, Chaplin DJ, May C, Rafii S. Combretastatin A4 phosphate induces rapid regression of tumor neovessels and growth through interference with vascular endothelial-cadherin signaling. J Clin Invest. 2005 Nov;115(11):2992-3006.
| Cas No. | 168555-66-6 | SDF | |
| 别名 | CA 4DP; CA 4P; Combretastatin A4 disodium phosphate | ||
| 化学名 | disodium;[2-methoxy-5-[(Z)-2-(3,4,5-trimethoxyphenyl)ethenyl]phenyl] phosphate | ||
| Canonical SMILES | COC1=C(C=C(C=C1)C=CC2=CC(=C(C(=C2)OC)OC)OC)OP(=O)([O-])[O-].[Na+].[Na+] | ||
| 分子式 | C18H19Na2O8P | 分子量 | 440.29 |
| 溶解度 | ≥ 11.7mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2712 mL | 11.3562 mL | 22.7123 mL |
| 5 mM | 0.4542 mL | 2.2712 mL | 4.5425 mL |
| 10 mM | 0.2271 mL | 1.1356 mL | 2.2712 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet