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CAS NO.1492952-76-7
| Объект | Подробнее |
| Химическое название | Асциминиб |
| Номер по CAS | 1329068 - 34 - 4 |
| Молекулярная формула | \(C_{26}H_{23}N_{5}O_{2}\) |
| Молекулярная масса | 431.49 |
| Молекулярная структура | Asciminib has a unique structure with a central bicyclic heterocycle. It contains a quinazoline – like core with various substituents, including aromatic rings and nitrogen – containing side chains. This structure allows it to bind to the ABL1 kinase in a distinct way compared to traditional tyrosine kinase inhibitors. |
| Внешний вид | Usually appears as a solid, likely in a white to off – white powder form, though this can vary based on formulation. |
| Растворимость | Similar to many drugs in this class, it likely has limited solubility in water. It may have better solubility in organic solvents such as ethanol or DMSO. Solubility characteristics are important for developing effective pharmaceutical formulations, often requiring techniques to enhance solubility for optimal drug delivery. |
| Фармакологический класс | Kinase inhibitor (specifically, an allosteric inhibitor of ABL1 kinase) |
| Механизм действия | Asciminib binds to an allosteric site on the ABL1 kinase, which is different from the ATP – binding site targeted by most other tyrosine kinase inhibitors. By binding to this allosteric site, it induces a conformational change in the kinase, inhibiting its activity. In chronic myeloid leukemia (CML), the BCR – ABL1 fusion protein leads to abnormal activation of the ABL1 kinase. Asciminib’s unique mechanism of action can inhibit this abnormal kinase activity, even in cases where there are mutations in the ATP – binding site that cause resistance to traditional tyrosine kinase inhibitors. |
| Медицинские применения | Хронический миелоидный лейкоз: Approved for the treatment of adults with chronic – phase chronic myeloid leukemia (CP – CML) who are resistant or intolerant to two or more tyrosine kinase inhibitors. It has shown promise in providing an alternative treatment option for patients who have exhausted other treatment possibilities. By inhibiting the BCR – ABL1 kinase activity, it can reduce the number of leukemia cells in the body and potentially improve the patient’s prognosis. |
| Стабильность | Stable under normal storage conditions, typically at room temperature in a dry and dark environment. However, exposure to high humidity, extreme temperatures, or strong chemical agents can potentially cause degradation, which may affect its potency and safety. |
| Вопросы безопасности | Common side effects may include upper respiratory tract infections, headache, fatigue, and nausea. There is also a risk of cytopenias (low blood cell counts), such as neutropenia and thrombocytopenia, which can increase the risk of infections and bleeding. As with many drugs, it may interact with other medications. Drugs that affect the cytochrome P450 enzyme system, for example, can potentially impact the metabolism of Asciminib, leading to changes in its blood levels and the risk of adverse effects. |
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