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Fosbretabulin(Combretastatin A4 Phosphate(CA4P))Disodium
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Fosbretabulin(Combretastatin A4 Phosphate(CA4P))Disodium图片
CAS NO:168555-66-6
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
50mg电议

产品介绍
Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium (CA 4DP) 是一种微管蛋白去稳定剂。 Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium 是 Combretastatin A4 前药，可选择性靶向内皮细胞，诱导新生肿瘤新血管消退，减少肿瘤血流并导致中央肿瘤坏死。
Cas No.168555-66-6
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 SMILESCOC1=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 tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.