[Overview]
Combretastatin A4 (CA4) is a new type of vascular inhibitor with a similar structure to colchicine and similar targets. It targets tubulin in the body, inhibits its polymerization, and further selectively It destroys the vascular endothelial cells of tumor tissue and closes the blood vessels of tumor tissue, causing the tumor to lack oxygen and nutrients, thereby playing an anti-tumor effect. It has broad-spectrum anti-cancer cell activity and is highly cytotoxic to a variety of colon cancer cells, lung cancer cells, breast cancer cells, mouse leukemia cells and human malignant B lymphocytes. It is a new type of anti-tumor drug. However, its water solubility is extremely poor, only 11.8 μg/mL, resulting in low oral bioavailability, weakening its anti-tumor activity, and limiting clinical application.
[Physical and chemical properties]
Appearance and properties: Crystalline powder Vapor pressure: 3.09E-10mmHg at 25°C Refractive index: 1.607 Flash point: 250.3°C Melting point: 84.5-85.5oC Boiling point: 490.3°C at 760 mmHg Density: 1.184 g/cm3 [Pharmacological effects] It has the effects of inhibiting angiogenesis, inhibiting tumor growth, and anti-cancer
【Mechanism of action】
CA4 targets tubulin in vivo, inhibits its polymerization, and further destroys tumor blood vessels, thus exerting anti-tumor effects and is effective in a variety of tumor models. CA4 has little effect on normal cells, but selectively destroys tumor tissue vascular endothelial cells, causing tumor tissue blood vessels to close, resulting in tumor hypoxia and hypoxia.
[Preparation method]
Figure 1 shows the synthesis route of comprestin 1
Figure 2 shows the synthesis route 2 of Comprestin
[Purpose]
Used for content determination, identification, pharmacological experiments, etc.
