BRAF V600E Inhibitor HLX208

Preferred Label : BRAF V600E Inhibitor HLX208;

NCIt synonyms : BRAF (V600E) Inhibitor HLX208;

NCIt definition : An orally bioavailable, small molecule inhibitor of the v-raf murine sarcoma viral oncogene homolog B1 (BRAF) mutant V600E, with potential antineoplastic activity. Upon oral administration, BRAF V600E inhibitor HLX208 selectively binds to and inhibits the activity of BRAF V600E kinase, which may result in the inhibition of an over-activated MAPK signaling pathway downstream in BRAF(V600E) kinase-expressing tumor cells and a reduction in tumor cell proliferation. BRAF belongs to the raf/mil family of serine/threonine protein kinases and plays a role in regulating the MAP kinase/ERKs signaling pathway. The valine to glutamic acid substitution at residue 600 accounts for the majority of BRAF gene mutations. The oncogenic product, BRAF(V600E) kinase, exhibits a markedly elevated activity that over-activates the MAPK signaling pathway.;

Molecule name : HLX-208; HLX 208;

NCI Metathesaurus CUI : CL1770682;

Details

Origin ID

C182071;

UMLS CUI

C5666876;

Semantic type(s)
- Organic Chemical [UMLS semantic type]
- Pharmacologic Substance [UMLS semantic type]
chemical_or_drug_has_mechanism_of_action
- Enzyme Inhibition [NCIt concept]
chemical_or_drug_has_physiologic_effect
- Inhibition of Cell Proliferation [NCIt concept]
- Positive Regulation of Apoptosis [NCIt concept]
concept_is_in_subset
- GDC Terminology [NCIt concept]
- GDC Therapeutic Agent Terminology [NCIt concept]
- NCI Drug Dictionary Terminology [NCIt concept]
- NCIt Antineoplastic Agent Terminology [NCIt concept]
has_target
- Serine/Threonine-Protein Kinase B-Raf [NCIt concept]

Keyword's position in hierarchy(ies) :

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