AG-1024 (Selective IGF-1R inhibitor AG1024, CAS: 65678-07-1) is a small-molecule inhibitor of the insulin-like growth factor-1 receptor (IGF-1R) developed by Pfizer for the treatment of various cancers. IGF-1R is a tyrosine kinase that plays a crucial role in cell proliferation, survival, and differentiation.
Chemical name: N-(4-(3-bromophenyl)-2-thiazolyl)-2-methylbenzenesulfonamide
Molecular formula: C15H12BrN3O2S2
Formula weight: 447.31 g/mol
CAS No: 65678-07-1
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Health benefits of this product: AG-1024 has shown potential in preclinical and clinical studies for the treatment of various cancers, such as breast, prostate, and lung cancers. It works by inhibiting the activity of IGF-1R, which promotes cancer cell proliferation, survival, and differentiation. By blocking IGF-1R, AG-1024 can potentially reduce cancer cell growth and induce apoptosis, or programmed cell death.
Potential effects: AG-1024 has shown promising anti-tumor activity in preclinical and clinical studies. In particular, it has demonstrated efficacy in reducing tumor growth and inducing remission in breast, prostate, and lung 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: AG-1024 works by inhibiting the activity of IGF-1R, which is involved in the regulation of cell proliferation, survival, and differentiation. Overexpression of IGF-1R is associated with various cancers, including breast, prostate, and lung cancers. As a tyrosine kinase inhibitor, AG-1024 binds to the ATP-binding site of IGF-1R, preventing its activation and downstream signaling pathways that promote cancer cell growth and survival. By inhibiting IGF-1R, AG-1024 can block cancer cell growth and induce apoptosis.
Safety: AG-1024 has been evaluated in several preclinical and clinical studies involving hundreds of patients with different types of cancers. Overall, it has been well-tolerated, with manageable side effects. The most common adverse events reported were nausea, vomiting, diarrhea, fatigue, and headache. More severe side effects, such as thrombocytopenia and liver toxicity, were observed in some patients, but they were rare and usually resolved after dose adjustments or discontinuation.
Side effects: Common side effects of AG-1024 include nausea, vomiting, diarrhea, fatigue, and headache. 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 thrombocytopenia and liver toxicity, 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 AG-1024 varies depending on the indication and the patient's condition. In clinical trials, doses ranging from 100 to 300 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: AG-1024 is a promising small-molecule inhibitor of IGF-1R that has shown potential in preclinical and clinical studies for the treatment of various cancers, such as breast, prostate, and lung cancers. Its mechanism of action involves blocking key receptors involved in cancer cell growth and survival, 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 cancers.
