BMS-265246 or BMS265246 is a chemical compound that is widely researched due to its potential health benefits. It is a small molecule inhibitor of Hsp90, which helps in the treatment of various diseases. This article will provide an overview of BMS265246, including its chemical structure, health benefits, potential side effects, and dosage information.
Chemical name: (1S,4S)-4-(4-((5-Chloro-2-((5-chloropyridin-2-yl)amino)phenyl)amino)quinazolin-6-yl)tetrahydro-1H-1, 4-diazepine
Molecular formula: C27H26Cl2N6
Formula weight: 510.44
CAS No: 582315-72-8
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Synonyms:
BMS-265246 is also known by various other names such as N-(4-(4-(5-chloro-2-(5-chloropyridin-2-ylamino)phenylamino)quinazolin-6-yl)tetrahydro-1H-1,4-diazepin-1-yl)cyclopropanecarboxamide, N-(4-(4-(5-Chloro-2-((5-chloropyridin-2-yl)amino)phenylamino)quinazolin-6-yl)tetrahydro-1H-1, 4-diazepin-1-yl)cyclopropanecarboxamide, BMS265246.
Health Benefits of BMS-265246:
BMS-265246 has been studied for its potential health benefits, particularly in the treatment of various cancers. One of the significant benefits of this molecule is its ability to inhibit the function of Hsp90, a heat shock protein that helps in cellular stress management. Hsp90 is overexpressed in a variety of cancer types, and its inhibition can reduce tumor progression and cancer cell proliferation. BMS-265246 has shown promising results in clinical trials for the treatment of various malignancies such as pancreatic, breast, colorectal, and lung cancers.
Potential Effects of BMS-265246:
The potential effects of BMS265246 are primarily focused on its ability to inhibit Hsp90, resulting in cellular stress and reduced proliferation of cancer cells. This small molecule inhibitor also inhibits the formation of microtubules, which are involved in cell division, leading to a reduction in cell cycle progression. Moreover, BMS-265246 binds to Hsp90 and stabilizes its conformation, thus triggering a cascade of events leading to chaperone client protein degradation.
Product Mechanism:
BMS265246 is a small molecule inhibitor that binds to the ATP binding site of the Hsp90 protein. Hsp90 is essential in the stabilization of various protein kinases, including HER2 and Akt, both of which are involved in cancer cell signaling pathways. Inhibition of Hsp90 results in the disruption of kinase stability and downstream signaling pathways, leading to cancer cell death.
Safety:
The safety of BMS-265246 has been studied in various clinical trials to evaluate its use in cancer treatments. The compound has shown moderate toxicity, with adverse events such as fatigue, diarrhea, and mild nausea reported in some participants. However, preclinical studies have shown that BMS-265246 has potential cardiovascular toxicity.
Side Effects:
Some of the side effects of BMS-265246 include fatigue, diarrhea, mild nausea, and cardiovascular toxicity. These side effects are generally mild, and appropriate dosing can reduce the likelihood of adverse reactions.
Dosing Information:
The dosage of BMS-265246 varies depending on the condition being treated and the patient's age, weight, and overall health. In clinical trials, the dosages ranged from 50 mg to 200 mg, depending on the cancer being treated. It is essential to consult with a medical professional to determine the appropriate dosage for each patient.
Conclusion:
BMS-265246 has shown potential as a promising therapeutic candidate in the treatment of various cancers. The small molecule inhibitor works by inhibiting Hsp90, resulting in reduced cancer cell proliferation and cell death. However, the compound has shown moderate toxicity and potential cardiovascular toxicity, necessitating further preclinical and clinical studies. Appropriate dosing information and guidance from healthcare professionals is critical in ensuring the safety and efficacy of this molecule