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MK-8745
- Development stage
- Discontinued
- Lead developer
- Merck
- Modality
- Small Molecules
- Administration
- Subcutaneous, Parenteral
01
Overview
MK-8745 is a potent, selective, small-molecule inhibitor of Aurora A kinase (IC50 = 0.6 nM), demonstrating over 450-fold selectivity for Aurora A over Aurora B. Developed by Merck & Co., the compound acts as a research tool to study mitotic processes and cell cycle regulation. Inhibition of Aurora A by MK-8745 leads to G2/M cell cycle arrest, accumulation of tetraploid nuclei, and apoptotic cell death in a p53-dependent manner. It has been investigated preclinically in various cancer models, including non-Hodgkin lymphoma, breast cancer, colon cancer, sarcoma, melanoma, and pancreatic cancer.
- Other names
- (3-chloro-2-fluorophenyl)(4-((6-(thiazol-2-ylamino)pyridin-2-yl)methyl)piperazin-1-yl)methanone(3-chloro-2-fluorophenyl)[4-[[6-(2-thiazolylamino)-2-pyridinyl]methyl]-1-piperazinyl]-methanone
02
Targets
AURKA (Aurora kinase A)AURKB (Aurora kinase B)
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