#152625

Mps1 inhibitor CCT251455 Small Molecule (Tool Compound)

Please Enter Your Email ID
Email ID

Cat. #152625

Mps1 inhibitor CCT251455 Small Molecule (Tool Compound)

Cat. #: 152625

Sub-type: Inhibitor

Availability: Please enquire for quantities and pricing

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%.

This fee is applicable only for non-profit organisations. If you are a for-profit organisation or a researcher working on commercially-sponsored academic research, you will need to contact our licensing team for a commercial use license.

Contributor

Inventor: Julian Blagg

Institute: The Institute of Cancer Research

Tool Details
Handling
Target Details
Application Details
References

Tool Details

*FOR RESEARCH USE ONLY

  • Tool name: Mps1 inhibitor CCT251455 Small Molecule (Tool Compound)
  • Research fields: Cancer
  • Molecular formula: C26H26ClN7O2
  • Tool sub type: Inhibitor
  • Primary target: Monopolar spindle 1 (Mps1, also known as TTK)
  • 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.
  • 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
  • Additional notes: Published poster at the 2012 AACR meeting: http://cancerres.aacrjournals.org/content/72/8_Supplement/1817.short

Handling

  • Purity: 503.99 g/mol
  • Shipping conditions: Dry Ice

Target Details

  • Primary target: Monopolar spindle 1 (Mps1, also known as TTK)
  • 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.

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%.

References

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