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Version: 17.10e (Release date: 2017-10-30)
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Vemurafenib (Code C64768)

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Terms & Properties

Preferred Name: Vemurafenib

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.

NCI-GLOSS Definition: 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.

Display Name: Vemurafenib

Label: Vemurafenib

NCI Thesaurus Code: C64768 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C1832009  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
1-propanesulfonamide, n-(3-((5-(4-chlorophenyl)-1h-pyrrolo(2,3-b)pyridin-3-yl)carbonyl)-2,4-difluorophenyl)-
BRAF (V600E) kinase inhibitor RO5185426
BRAF(V600E) Kinase Inhibitor RO5185426
RG 7204
RO 5185426

External Source Codes: 
CAS Registry Number 918504-65-1 (see NLM ChemIDplus info)
ChEBI ID CHEBI:63637 (see ChEBI info)
PDQ Closed Trial Search ID 528954
PDQ Open Trial Search ID 528954 (check for NCI PDQ open clinical trial info)
UMLS CUI C1832009

Other Properties:
     Name Value (qualifiers indented underneath)
Accepted_Therapeutic_Use_For Advanced Melanoma
Chemical_Formula C23H18ClF2N3O3S
code C64768
Contributing_Source CTRP
Contributing_Source FDA
Legacy_Concept_Name PLX4032
Semantic_Type Organic Chemical
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  


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