MLchartDataset catalogue

RAF inhibitor DCC-3084

Term · Oncology and biomedicine · MLC-T-ONC-016350

An orally bioavailable central nervous system (CNS)-penetrant switch control inhibitor of the serine/threonine protein kinase Raf family, with potential antineoplastic activity. Upon oral administration, RAF inhibitor DCC-3084 targets and binds to BRAF and CRAF kinases, including BRAF monomeric class I mutation, dimeric class II (Ras-independent) and class III (Ras-dependent) mutations, BRAF fusions and BRAF/CRAF heterodimers, specifically at the switch pocket regions, thereby binding both monomers of the RAF dimers and preventing paradoxical activation that results from unbound monomers. This prevents the activation of Raf-mediated signal transduction pathways, which may inhibit tumor cell growth. Raf protein kinases are critical enzymes in the Ras/Raf/MEK/ERK signaling pathway and are upregulated in a variety of cancer cell types. They play key roles in tumor cell proliferation and survival.

Table 1. Record
IdentifierMLC-T-ONC-016350
FieldOncology and biomedicine
SynonymsBRAF/CRAF inhibitor DCC-3084; RAF dimer inhibitor DCC-3084
ReferencesNational Cancer Institute Thesaurus (CC BY 4.0)
Record as JSON
{
  "id": "MLC-T-ONC-016350",
  "term": "RAF inhibitor DCC-3084",
  "field": "Oncology and biomedicine",
  "definition": "An orally bioavailable central nervous system (CNS)-penetrant switch control inhibitor of the serine/threonine protein kinase Raf family, with potential antineoplastic activity. Upon oral administration, RAF inhibitor DCC-3084 targets and binds to BRAF and CRAF kinases, including BRAF monomeric class I mutation, dimeric class II (Ras-independent) and class III (Ras-dependent) mutations, BRAF fusions and BRAF/CRAF heterodimers, specifically at the switch pocket regions, thereby binding both monomers of the RAF dimers and preventing paradoxical activation that results from unbound monomers. This prevents the activation of Raf-mediated signal transduction pathways, which may inhibit tumor cell growth. Raf protein kinases are critical enzymes in the Ras/Raf/MEK/ERK signaling pathway and are upregulated in a variety of cancer cell types. They play key roles in tumor cell proliferation and survival.",
  "synonyms": [
    "BRAF/CRAF inhibitor DCC-3084",
    "RAF dimer inhibitor DCC-3084"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/raf-inhibitor-dcc-3084/"
}

Record 14,042 of 17,717 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.