PHA-739358 (Danusertib, PHA739358, CAS: 827318-97-8) is a small molecule inhibitor of Aurora kinases A and B, which are enzymes involved in the regulation of cell division. It has been investigated as a potential therapeutic agent for cancer, particularly in the treatment of acute myeloid leukemia (AML) and advanced solid tumors.
Chemical name: 4-((7-(3-(dimethylamino)propoxy)-2-oxo-2H-chromen-4-yl)amino)-3-phenylbut-2-enoic acid
Molecular formula: C29H31N3O5
Formula weight: 505.58 g/mol
CAS No: 827318-97-8
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Health benefits of this product: PHA-739358 has demonstrated potential health benefits in the area of cancer research, particularly in the treatment of AML and advanced solid tumors. Its primary mode of action is through inhibition of Aurora kinases A and B, leading to disruption of mitotic spindle formation and subsequent cell division.
Potential effects: PHA-739358 has demonstrated efficacy in several preclinical and clinical studies in inhibiting the activity of Aurora kinases A and B, leading to disrupted mitotic spindle formation and subsequent cell division. It also has potential benefits for inducing apoptosis (programmed cell death), reducing angiogenesis (the formation of new blood vessels that can support tumor growth), and inhibiting signal transduction pathways that regulate cell survival and proliferation. PHA-739358 works by disrupting various cellular processes that are necessary for cancer cell survival and growth.
Product mechanism: PHA-739358 works by inhibiting the activity of Aurora kinases A and B, which are enzymes involved in the regulation of cell division. By inhibiting these enzymes, PHA-739358 can disrupt mitotic spindle formation and subsequent cell division, leading to reduced tumor growth and increased apoptosis.
Safety: PHA-739358 has been evaluated in several preclinical and clinical trials involving hundreds of participants and has been generally well-tolerated. Rare but potential side effects may include gastrointestinal symptoms such as nausea, vomiting, and diarrhea, as well as hematological abnormalities (e.g., decreased white blood cell or platelet counts) and hepatic dysfunction. Patients with liver or kidney disease should exercise caution when taking PHA-739358, as it may affect these conditions. Pregnant or breastfeeding women should avoid using PHA-739358, as its safety in these populations has not been established.
Side effects: Common side effects of PHA-739358 may include gastrointestinal symptoms such as nausea, vomiting, and diarrhea. 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 disorders, cardiovascular events, and liver or kidney dysfunction, 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 optimal dose and dosing regimen of PHA-739358 may vary depending on the patient's condition and treatment goals. In preclinical studies, doses ranging from 10 to 200 mg have been evaluated for various types of cancer. Patients should follow their doctor's instructions regarding dosing, administration, and monitoring.
Conclusion: PHA-739358 (Danusertib, PHA739358, CAS: 827318-97-8) is a small molecule inhibitor of Aurora kinases A and B, which are enzymes involved in the regulation of cell division. It has been investigated as a potential therapeutic agent for cancer, particularly in the treatment of AML and advanced solid tumors. Although it has been generally well-tolerated in preclinical and clinical trials, it may cause some side effects that should be monitored closely. More research is needed to determine its full potential and efficacy in different patient populations and cancer types. PHA-739358 offers a promising avenue for treatment of cancer by disrupting mitotic spindle formation and inhibiting tumor growth
