Mps1 inhibitor CCT251455 Small Molecule (Tool Compound)

A potent and selective chemical tool that stabilizes an inactive conformation of MPS1. MPS1 is a crucial component of the spindle assembly checkpoint signal and is aberrantly overexpressed in many human cancers.

Contributors

Inventor Institute
Julian Blagg The Institute of Cancer Research
Cat. #: 152625
Tool sub type: Inhibitor
Research Fields: Cancer
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%.
Purpose: Inhibitor
Product 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.
Additional notes: Published poster at the 2012 AACR meeting: http://cancerres.aacrjournals.org/content/72/8_Supplement/1817.short
Primary target: Monopolar spindle 1 (Mps1, also known as TTK)
Shipping conditions: Dry Ice
References:

J. Med. Chem. 2013, 56, 10045-10065. PMID: 24256217

Images

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Molecular structure of CCT251455.

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