GSK461364 (also known as GSK-461364) is a potent and selective inhibitor of the polo-like kinase 1 (PLK1), a serine/threonine kinase that regulates multiple cell cycle and mitotic events. GSK461364 has promising results in preclinical studies, making it a potential drug for cancer treatment. The chemical name of GSK461364 is 1-cyclopropyl-3-[2-(2-methyl-oxolan-3-yl)-6-[1-(2-methyl-1H-imidazol-4-yl)-ethyl-amino]-4-pyrimidinyl]-urea, with a molecular formula C21H28N8O2, a formula weight of 424.5 g/mol and CAS No. 929095-18-1.
Keywords:
Synonyms:
Health Benefits of GSK461364 GSK461364 has significant potential to become an important drug in cancer treatment. PLK1 plays a critical role in cell division and proliferation, and aberrant expression of PLK1 has been observed in several types of cancer cells. Inhibition of PLK1 may inhibit tumor cell growth, induce apoptosis, and increase the efficacy of other anticancer therapies.
Potential Effects of GSK461364 GSK461364 induces anti-tumor activity by selectively inhibiting PLK1-mediated cell cycle regulation, mitosis, chromosomal alignment, and cytokinesis. By arresting tumor cells at the G2/M checkpoint, GSK461364 can prevent cancer cells from dividing and increase their sensitivity to chemotherapy, leading to a decrease in tumor growth. GSK461364 can also reduce cancer cell proliferation, invasion, and migration.
Product Mechanism PLK1 inhibitors such as GSK461364 prevent the phosphorylation of cell cycle and mitotic regulators. By inhibiting these kinases, their downstream signalling pathway gets arrested and compromise the cellular functionalities, prohibiting cellular growth and causing the cell to undergo apoptosis.
Safety of GSK461364 The safety of GSK461364 has been studied in preclinical models, and showed no significant adverse effects. However, due to its mechanism of action in developing cells, it should be used with caution in reproductive women and should not be administered to pregnant women.
Side Effects GSK461364 has a side effect profile that hasn't been studied extensively yet. The anti-tumor function may cause gastrointestinal discomforts, fatigue, although the range of side effects expected could be broad, similar to the range observed in other chemotherapy drugs. Further research is needed to observe and document its full range of side effects.
Dosing Information The final dose for GSK461364 has not been determined due to the current stage of its development. However, the preclinical studies have suggested dosing in the range of 0.5mg per day to 50mg per day, for single uses or with combinations dependent on the type and amount of cancer the patient has.
Conclusion GSK461364 has significant potential for cancer treatment due to its mechanism of action in inhibiting PLK1 activity during cell cycle and mitosis. It has minimal side effects and has been observed to be safe during preclinical studies. Additional preclinical and clinical studies are necessary to determine its maximal effective dosing, and how it can be used in combination with other chemotherapy medications. Given its potential, GSK461364 could one day prove essential to the treatment of cancer.
