MPI-0479605 Chemical Structure
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MPI-0479605 is a potent and selective ATP competitive inhibitor of Mps1. Cells treated with MPI-0479605 undergo aberrant mitosis, resulting in aneuploidy and formation of micronuclei. In cells with wild-type p53, this promotes the induction of a postmitotic checkpoint characterized by the ATM- and RAD3-related-dependent activation of the p53-p21 pathway. In both wild-type and p53 mutant cells lines, there is a growth arrest and inhibition of DNA synthesis. Subsequently, cells undergo mitotic catastrophe and/or an apoptotic response. In xenograft models, MPI-0479605 inhibits tumor growth, suggesting that drugs targeting Mps1 may have utility as novel cancer therapeutics.
Mol. Formula: C22H29N7O
Chiral Purity: 100%
Canonical SMILES: CC1=CC(N2CCOCC2)=CC=C1NC3=NC(NC4CCCCC4)=C5N=CNC5=N3
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