SU5416

SU5416 is a synthetic compound that acts as a vascular endothelial growth factor receptor (VEGFR) inhibitor. It is primarily used in scientific research to study the role of VEGFR in various biological processes and diseases, including cancer and angiogenesis.

Chemistry

SU5416 is a small molecule with a molecular weight of 294.3 g/mol. It is a semi-synthetic derivative of indolinone, a class of compounds known for their potent inhibitory activity against tyrosine kinases. The compound is highly selective for VEGFR, particularly VEGFR-2, which is the primary receptor involved in angiogenesis.

Mechanism of Action

SU5416 exerts its effects by binding to the ATP-binding site of VEGFR, thereby preventing the receptor from being activated by its natural ligand, vascular endothelial growth factor (VEGF). This inhibits the downstream signaling pathways that are involved in cell proliferation and angiogenesis.

Applications in Research

In the field of cancer research, SU5416 is often used to study the role of angiogenesis in tumor growth and metastasis. By inhibiting VEGFR, SU5416 can effectively block the formation of new blood vessels, thereby starving the tumor of the nutrients it needs to grow.

In addition to its use in cancer research, SU5416 has also been used to study other diseases that involve abnormal angiogenesis, such as macular degeneration and rheumatoid arthritis.

Clinical Trials

Several clinical trials have been conducted to evaluate the potential use of SU5416 as a therapeutic agent in various types of cancer. However, the results have been mixed, with some studies showing promising results and others showing no significant benefit. Further research is needed to fully understand the potential therapeutic applications of SU5416.

Safety and Toxicity

Like all drugs, SU5416 has the potential to cause side effects. The most common side effects observed in clinical trials include fatigue, nausea, and diarrhea. In some cases, SU5416 can also cause more serious side effects, such as liver damage and heart problems.

See Also

• Angiogenesis
• Vascular endothelial growth factor
• Vascular endothelial growth factor receptor
• Cancer
• Indolinone

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