Mps1 inhibitor CCT251455 Small Molecule (Tool Compound)
- Name Julian Blagg
- Institute The Institute of Cancer Research
Tool name: Mps1 inhibitor CCT251455 Small Molecule (Tool Compound)
Molecular formula: C26H26ClN7O2
Tool type: Small molecules
Tool sub-type: Inhibitor
Application: CCT251455 displays a favorable oral pharmacokinetic profile, shows dose-dependent inhibition of MPS1 in an HCT116 human tumor xenograft model, and is an attractive tool compound to elucidate further the therapeutic potential of MPS1 inhibition. In Female Balb/C mice it had an oral bioavailabilty of 83%.
Description: The Mps1 inhibitor CCT251455 is a potent and selective chemical tool stabilizes an inactive conformation of MPS1 with the activation loop ordered in a manner incompatible with ATP and substrate-peptide binding. MPS1 is a crucial component of the spindle assembly checkpoint signal and is aberrantly overexpressed in many human cancers.
Research area: Cancer
IC50: IC50 of 0.003uM in MPS1 assay, p-MPS1 Cell Assay IC50 of 0.04uM and a GI50 of 0.16uM in HT-116 Human Colon Cancer cell line.
Additional notes: Published poster at the 2012 AACR meeting: http://cancerres.aacrjournals.org/content/72/8_Supplement/1817.short
- For Research Use Only
- • J. Med. Chem. 2013, 56, 10045-10065. PMID: 24256217