Preferred Label : Vemurafenib;
NCIt synonyms : BRAF(V600E) Kinase Inhibitor RO5185426; 1-propanesulfonamide, n-(3-((5-(4-chlorophenyl)-1h-pyrrolo(2,3-b)pyridin-3-yl)carbonyl)-2,4-difluorophenyl)-;
NCIt related terms : BRAF (V600E) kinase inhibitor RO5185426; RG7204; PLX4032;
NCIt definition : An orally bioavailable, ATP-competitive, small-molecule inhibitor of BRAF(V600E) kinase
with potential antineoplastic activity. Vemurafenib selectively binds to the ATP-binding
site of BRAF(V600E) kinase and inhibits its activity, which may result in an inhibition
of an over-activated MAPK signaling pathway downstream in BRAF(V600E) kinase-expressing
tumor cells and a reduction in tumor cell proliferation. Approximately 90% of BRAF
gene mutations involve a valine-to-glutamic acid mutation at residue 600 (V600E);
the oncogene protein product, BRAF(V600E) kinase, exhibits a markedly elevated activity
that over-activates the MAPK signaling pathway. The BRAF(V600E) gene mutation has
been found to occur in approximately 60% of melanomas, and in about 8% of all solid
tumors, including melanoma, colorectal, thyroid and other cancers.;
Alternative definition : NCI-GLOSS: A substance being studied in the treatment of cancer. BRAF (V600E) kinase
is a mutated (changed) form of a cell protein called BRAF. It is found in several
types of cancer, including melanoma (a type of skin cancer). Inhibiting this kinase
may cause cancer cells to die. BRAF (V600E) kinase is a type of serine/threonine kinase
inhibitor and a type of targeted therapy agent.;
UNII : 207SMY3FQT;
InChIKey : GPXBXXGIAQBQNI-UHFFFAOYSA-N;
CAS number : 918504-65-1;
Drug name : Zelboraf;
Molecule name : RO-5185426; RG 7204; RO 5185426; PLX-4032; RG-7204; PLX 4032;
Chemical formula : C23H18ClF2N3O3S;
ChEBI ID : CHEBI:63637;
Codes from synonyms : CDR0000670004; CDR0000670003; CDR0000670002; 533;
Origin ID : C64768;
UMLS CUI : C3192263;
Automatic exact mappings (from CISMeF team)
- Currated CISMeF NLP mapping
- See also inter- (CISMeF)
- Semantic type(s)
- UMLS correspondences (same concept)
- chemical_or_drug_has_mechanism_of_action
- chemical_or_drug_has_physiologic_effect
- concept_is_in_subset
- has_target
- is_component_of_chemotherapy_regimen
