MLchartDataset catalogue

threonine tyrosine kinase inhibitor CFI-402257

Term · Oncology and biomedicine · MLC-T-ONC-017150

An orally bioavailable, selective inhibitor of the dual specificity protein kinase TTK (monopolar spindle 1 kinase, Mps1), with potential antineoplastic activity. Upon administration, luvixasertib selectively binds to and inhibits the activity of Mps1. This inactivates the spindle assembly checkpoint (SAC) and accelerates mitosis, which results in chromosomal misalignment and missegregation, and mitotic checkpoint complex destabilization. This induces cell death in Mps1-overexpressing cancer cells. Mps1, a tyrosine and serine/threonine kinase expressed in proliferating normal tissues, is essential for proper SAC functioning and chromosome alignment. Overexpressed in various human tumors, Mps1 plays a key role in uncontrolled tumor cell growth.

Table 1. Record
IdentifierMLC-T-ONC-017150
FieldOncology and biomedicine
SynonymsTTK inhibitor CFI-402257; MSP1 inhibitor CFI-402257
ReferencesNational Cancer Institute Thesaurus (CC BY 4.0)
Record as JSON
{
  "id": "MLC-T-ONC-017150",
  "term": "threonine tyrosine kinase inhibitor CFI-402257",
  "field": "Oncology and biomedicine",
  "definition": "An orally bioavailable, selective inhibitor of the dual specificity protein kinase TTK (monopolar spindle 1 kinase, Mps1), with potential antineoplastic activity. Upon administration, luvixasertib selectively binds to and inhibits the activity of Mps1. This inactivates the spindle assembly checkpoint (SAC) and accelerates mitosis, which results in chromosomal misalignment and missegregation, and mitotic checkpoint complex destabilization. This induces cell death in Mps1-overexpressing cancer cells. Mps1, a tyrosine and serine/threonine kinase expressed in proliferating normal tissues, is essential for proper SAC functioning and chromosome alignment. Overexpressed in various human tumors, Mps1 plays a key role in uncontrolled tumor cell growth.",
  "synonyms": [
    "TTK inhibitor CFI-402257",
    "MSP1 inhibitor CFI-402257"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/threonine-tyrosine-kinase-inhibitor-cfi-402257/"
}

Record 16,306 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.