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Version: 17.06d (Release date: 2017-06-26)
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BRAF(V600E) Kinase Inhibitor RO5212054 (Code C92591)

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Terms & Properties

Preferred Name: BRAF(V600E) Kinase Inhibitor RO5212054

Definition: An orally available small-molecule inhibitor of mutant (V600E) v-raf murine sarcoma viral oncogene homolog B1 (BRAF) with potential antineoplastic activity. BRAF(V600E) kinase inhibitor RO5212054 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. The valine to glutamic acid substitution at residue 600 accounts for about 90% of BRAF gene mutations; the oncogenic product, BRAF(V600E) kinase, exhibits a markedly elevated activity that over-activates the MAPK signaling pathway. The BRAF(V600E) mutation has been found to occur in approximately 60% of melanomas, and in about 8% of all solid tumors.

Label: BRAF(V600E) Kinase Inhibitor RO5212054

NCI Thesaurus Code: C92591 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: CL421616  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
B-Raf Inhibitor RO5212054
BRAF(V600E) Kinase Inhibitor RO5212054
PLX3603
RO5212054

External Source Codes: 
PDQ Closed Trial Search ID 680347
PDQ Open Trial Search ID 680347 (check for NCI PDQ open clinical trial info)
NCI META CUI CL421616

Other Properties:
     Name Value (qualifiers indented underneath)
code C92591
Semantic_Type Organic Chemical
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  

URL: https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C92591

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