MLchartDataset catalogue

rebastinib tosylate

Term · Oncology and biomedicine · MLC-T-ONC-016381

An orally bioavailable small-molecule inhibitor of multiple tyrosine kinases with potential antineoplastic activity. Rebastinib binds to and inhibits the Bcr-Abl fusion oncoprotein by changing the conformation of the folded protein to disallow ligand-dependent and ligand-independent activation; in addition, this agent binds to and inhibits Src family kinases LYN, HCK and FGR and the receptor tyrosine kinases TIE-2 and VEGFR-2. Rebastinib may exhibit more potent activity against T315I Bcr-Abl gatekeeper mutant kinases than other Bcr-Abl kinase inhibitors. The TIE-2 and VEGFR-2 receptor tyrosine kinases regulate angiogenesis, respectively, while the Src family kinases Abl, LYN, and HCK Src regulate a variety of cellular responses including differentiation, division, adhesion, and the stress response.

Table 1. Record
IdentifierMLC-T-ONC-016381
FieldOncology and biomedicine
Synonymsmultitargeted tyrosine kinase inhibitor DCC-2036
ReferencesNational Cancer Institute Thesaurus (CC BY 4.0)
Record as JSON
{
  "id": "MLC-T-ONC-016381",
  "term": "rebastinib tosylate",
  "field": "Oncology and biomedicine",
  "definition": "An orally bioavailable small-molecule inhibitor of multiple tyrosine kinases with potential antineoplastic activity. Rebastinib binds to and inhibits the Bcr-Abl fusion oncoprotein by changing the conformation of the folded protein to disallow ligand-dependent and ligand-independent activation; in addition, this agent binds to and inhibits Src family kinases LYN, HCK and FGR and the receptor tyrosine kinases TIE-2 and VEGFR-2. Rebastinib may exhibit more potent activity against T315I Bcr-Abl gatekeeper mutant kinases than other Bcr-Abl kinase inhibitors. The TIE-2 and VEGFR-2 receptor tyrosine kinases regulate angiogenesis, respectively, while the Src family kinases Abl, LYN, and HCK Src regulate a variety of cellular responses including differentiation, division, adhesion, and the stress response.",
  "synonyms": [
    "multitargeted tyrosine kinase inhibitor DCC-2036"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/rebastinib-tosylate/"
}

Record 14,111 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.