Mps1 inhibitor CCT251455 Small Molecule (Tool Compound)
Invented at The Institute of Cancer Research
- Datasheet
- References (2)
- Inventor Info
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: 2 entries
Naud et al. 2013. J Med Chem. 56(24):10045-65. PMID: 24256217.
Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1).
Europe PMC ID: 24256217
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References: 2 entries
Naud et al. 2013. J Med Chem. 56(24):10045-65. PMID: 24256217.
Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1).
Add a reference
