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Mps1 inhibitor CCT251455 Small Molecule (Tool Compound)

Info

Catalogue Number 152625
Antigen/Gene or Protein Targets Monopolar spindle 1 (Mps1, also known as TTK)
Type Inhibitor
Relevance 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.
On Target 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.
Molecular Formula C26H26ClN7O2
In vivo applications 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%.
Research Area Cell Cycle, Epigenetics & Nuclear Signalling
Notes Published poster at the 2012 AACR meeting: http://cancerres.aacrjournals.org/content/72/8_Supplement/1817.short

References: 1 entry

Naud et al. 2013. J Med Chem. 56(24):10045-65. PMID: 24256217.


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References: 1 entry

Naud et al. 2013. J Med Chem. 56(24):10045-65. PMID: 24256217.


Add a reference

References: 1 entry

Naud et al. 2013. J Med Chem. 56(24):10045-65. PMID: 24256217.


Add a reference


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