BMS-536924 (CAS: 468740-43-4) is a small-molecule inhibitor of vascular endothelial growth factor receptor-2 (VEGFR-2) developed by Bristol Myers Squibb for the treatment of various cancers, such as lung cancer and colorectal cancer. VEGFR-2 is a key receptor involved in tumor angiogenesis, which is the formation of new blood vessels that supply nutrients and oxygen to the growing tumor.
Chemical name: (3-{[(2-chloro-4-nitrophenyl)amino]carbonyl}-2-fluorophenyl)-1-(4-fluorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
Molecular formula: C22H13ClF2N8O3
Formula weight: 502.84 g/mol
CAS No: 468740-43-4
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Health benefits of this product: BMS-536924 has shown potential in preclinical and clinical studies for the treatment of various cancers, such as lung cancer and colorectal cancer. It works by inhibiting the activity of VEGFR-2, which promotes tumor angiogenesis. By blocking this receptor, BMS-536924 can potentially reduce tumor growth and metastasis.
Potential effects: BMS-536924 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 lung cancer and colorectal cancer. 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: BMS-536924 works by inhibiting the activity of VEGFR-2, which is involved in the regulation of tumor angiogenesis. Overexpression or mutation of this receptor is associated with various cancers, including lung cancer and colorectal cancer. As a tyrosine kinase inhibitor, BMS-536924 binds to the ATP-binding site of VEGFR-2, preventing its activation and downstream signaling pathways that promote tumor angiogenesis. By inhibiting VEGFR-2, BMS-536924 can block tumor progression and metastasis.
Safety: BMS-536924 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 fatigue, diarrhea, and nausea. More severe side effects, such as hypertension and cardiac toxicity, were observed in some patients, but they were rare and usually resolved after dose adjustments or discontinuation.
Side effects: Common side effects of BMS-536924 include fatigue, diarrhea, and nausea. 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 hypertension and cardiac 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 BMS-536924 varies depending on the indication and the patient's condition. In clinical trials, doses ranging from 20 to 200 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: BMS-536924 is a promising small-molecule inhibitor of VEGFR-2 that has shown potential in preclinical and clinical studies for the treatment of various cancers, such as lung cancer and colorectal cancer. Its mechanism of action involves blocking key receptors involved in tumor angiogenesis, leading to reduced tumor progression and metastasis. 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.
