SU-11274

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SU-11274 is a small molecule inhibitor that specifically targets the c-Met receptor tyrosine kinase. It is primarily used in research settings to study the role of c-Met in various cancers and to explore potential therapeutic applications.

Mechanism of Action

SU-11274 functions by inhibiting the kinase activity of the c-Met receptor. The c-Met receptor, also known as the hepatocyte growth factor receptor (HGFR), is a proto-oncogene that, when activated, can lead to cellular processes such as proliferation, survival, and metastasis. By inhibiting c-Met, SU-11274 can disrupt these pathways, potentially leading to reduced tumor growth and metastasis.

Research and Applications

Research has shown that SU-11274 can effectively inhibit c-Met activity in various cancer cell lines, including those derived from lung cancer, breast cancer, and gastric cancer. Studies have demonstrated that treatment with SU-11274 can lead to decreased cell proliferation, increased apoptosis, and reduced metastatic potential in these cells.

Preclinical Studies

In preclinical models, SU-11274 has been used to investigate the role of c-Met in tumorigenesis. For example, in xenograft models of human cancer, SU-11274 treatment has resulted in significant tumor growth inhibition. These studies suggest that c-Met inhibitors like SU-11274 could be valuable in the development of targeted cancer therapies.

Potential Clinical Implications

While SU-11274 itself is not currently used in clinical settings, its role as a research tool has provided valuable insights into the potential of c-Met as a therapeutic target. Ongoing research is focused on developing more potent and selective c-Met inhibitors for clinical use.

Chemical Properties

SU-11274 is characterized by its chemical structure, which includes a quinazoline core substituted with methoxy and halogen groups. This structure is crucial for its ability to bind to the ATP-binding site of the c-Met kinase domain, thereby inhibiting its activity.

Safety and Toxicology

As a research compound, SU-11274 is primarily used in laboratory settings. Safety data is limited, and it is not approved for human use. Researchers handling SU-11274 should follow standard laboratory safety protocols.

Also see

• c-Met
• Tyrosine kinase inhibitors
• Cancer research
• Targeted therapy

Receptor Tyrosine Kinase Inhibitors

Name	Target	Indications	Notes
Imatinib	BCR-ABL	Chronic myeloid leukemia, Gastrointestinal stromal tumor	First approved RTK inhibitor
Erlotinib	EGFR	Non-small cell lung cancer, Pancreatic cancer	Used in combination with gemcitabine for pancreatic cancer
Sunitinib	VEGFR, PDGFR	Renal cell carcinoma, Gastrointestinal stromal tumor	Multi-targeted RTK inhibitor
Gefitinib	EGFR	Non-small cell lung cancer	First EGFR inhibitor approved
Sorafenib	VEGFR, RAF kinase	Hepatocellular carcinoma, Renal cell carcinoma	Also inhibits RAF kinases
Lapatinib	HER2/neu, EGFR	Breast cancer	Used in combination with capecitabine