pan-variant KIT inhibitor THE-630

{
  "id": "MLC-T-ONC-015824",
  "term": "pan-variant KIT inhibitor THE-630",
  "field": "Oncology and biomedicine",
  "definition": "An orally bioavailable pan-inhibitor of the mutated forms of the tumor-associated antigen (TAA) receptor tyrosine kinase mast/stem cell factor receptor c-Kit (SCFR), with potential antineoplastic activity. Upon oral administration, pan-variant KIT inhibitor THE-630 targets, binds to and inhibits the activity of all known, clinically relevant KIT activating and resistance mutations in gastrointestinal stromal tumors (GIST). More specifically, THE-630 inhibits the primary activating mutations deletion in Ex11 (Ex11Del) and insertion in Ex9 (Ex9Ins); the secondary resistance mutations, including the ATP binding pocket mutants V654A and T670I and the activation loop mutants D816G/H, D820A/G, N822K, Y823D, and A829P. This inhibits KIT-mediated signaling and the proliferation of tumor cells that overexpress c-Kit mutations. c-Kit is mutated in various tumor cell types and plays a key role in the regulation of cellular proliferation and resistance to chemotherapy.",
  "synonyms": [
    "T pan-KIT-mutant inhibitor THE-630",
    "KIT-mutant inhibitor THE-630",
    "pan-KIT inhibitor THE-630"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/pan-variant-kit-inhibitor-the-630/"
}