SMALL MOLECULES
Contributor Information
- Name Julian Blagg
- Institute The Institute of Cancer Research
Tool Details
- Tool name: Mps1 inhibitor CCT251455 Small Molecule (Tool Compound)
- Molecular formula: C26H26ClN7O2
- Tool type: Small molecules
- Tool sub-type: Inhibitor
- Purpose: 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
Target Details
- Primary target: Monopolar spindle 1 (Mps1, also known as TTK)
Application Details
- 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%.
Handling
- Purity: 503.99 g/mol
- Shipping conditions: Dry Ice
Documentation
- Available on request
Related Tools
References
- • J. Med. Chem. 2013, 56, 10045-10065. PMID: 24256217
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