OSI-930 (Kit VEGFR 2 inhibitor, OSI930, CAS: 728033-96-3) is a small-molecule inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR-2) developed by OSI Pharmaceuticals for the treatment of solid tumors, such as breast, lung, and colon cancers. VEGFR-2 is a key mediator of angiogenesis, or the formation of new blood vessels that supply nutrients and oxygen to tumors.
Chemical name: N-methyl-1-(3-(4-(pyrrolidin-1-yl)phenyl)thiophene-2-carbonyl)piperazine-2-carboxamide
Molecular formula: C23H29N3O2S
Formula weight: 409.56 g/mol
CAS No: 728033-96-3
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Health benefits of this product: OSI-930 has shown potential in preclinical and clinical studies for the treatment of various solid tumors, such as breast, lung, and colon cancers. It works by inhibiting the activity of VEGFR-2, which promotes angiogenesis and tumor growth. By blocking VEGFR-2, OSI-930 can potentially reduce the blood supply to tumors, leading to decreased tumor growth, invasion, and metastasis.
Potential effects: OSI-930 has shown promising anti-tumor activity in preclinical and clinical studies. In particular, it has demonstrated efficacy in reducing tumor growth and metastasis in breast, lung, and colon cancers. It has also shown potential in combination with other anti-cancer agents, such as chemotherapy and radiation therapy. However, more research is needed to determine its full potential and efficacy in different types of tumors.
Product mechanism: OSI-930 works by binding to the ATP-binding site of the VEGFR-2 kinase, preventing its activation and downstream signaling pathways that promote angiogenesis and tumor growth. Its main targets include the tyrosine kinase domains of VEGFR-2, which are crucial for its dimerization and activation. By inhibiting VEGFR-2, OSI-930 can block endothelial cell proliferation, migration, and tube formation, leading to reduced angiogenesis and tumor growth.
Safety: OSI-930 has been evaluated in several preclinical and clinical studies involving hundreds of patients with different types of solid tumors. Overall, it has been well-tolerated, with manageable side effects. The most common adverse events reported were fatigue, nausea, vomiting, diarrhea, and hypertension. More severe side effects, such as bleeding and thrombosis, were observed in some patients, but they were rare and usually resolved after dose adjustments or discontinuation.
Side effects: Common side effects of OSI-930 include fatigue, nausea, vomiting, diarrhea, and hypertension. These symptoms are usually mild or moderate and can be managed with supportive care or dose modifications. Less common but more severe side effects may include bleeding and thrombosis, which may require prompt medical intervention. Patients should be monitored closely for these adverse events and receive appropriate medical intervention if necessary.
Dosing information: The recommended dose of OSI-930 varies depending on the indication and the patient's condition. In clinical trials, doses ranging from 50 to 900 mg/day have been evaluated, either as a single agent or in combination with other drugs. Treatment duration also varies and can range from a few weeks to several months, depending on the response and tolerability. Patients should follow their doctor's instructions regarding dosing, administration, and monitoring.
Conclusion: OSI-930 is a promising small-molecule inhibitor of VEGFR-2 that has shown potential in preclinical and clinical studies for the treatment of various solid tumors, such as breast, lung, and colon cancers. Its mechanism of action involves blocking key receptors involved in angiogenesis and tumor growth, leading to reduced tumor progression. Although it has been generally well-tolerated, it may cause some side effects that should be monitored closely. Further research is needed to determine its full potential and efficacy in different types of solid tumors
