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Version: 17.12d (Release date: 2017-12-26)
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Selumetinib (Code C66939)

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Terms & Properties

Preferred Name: Selumetinib

Definition: An orally active, small molecule with potential antineoplastic activity. Selumetinib is an ATP-independent inhibitor of mitogen-activated protein kinase kinase (MEK or MAPK/ERK kinase) 1 and 2. MEK 1 and 2 are dual specificity kinases that are essential mediators in the activation of the RAS/RAF/MEK/ERK pathway, are often upregulated in various cancer cells, and are drivers of diverse cellular responses, including proliferation. Inhibition of both MEK1 and 2 by selumetinib prevents the activation of MEK1/2 dependent effector proteins and transcription factors, thereby leading to an inhibition of cellular proliferation in various cancers.

NCI-GLOSS Definition: A substance being studied in the treatment of several types of cancer. AZD6244 blocks proteins needed for cell growth and may kill cancer cells. It is a type of protein kinase inhibitor.

Display Name: Selumetinib

Label: Selumetinib

NCI Thesaurus Code: C66939 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C1832054  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
MEK inhibitor AZD6244
MEK Inhibitor AZD6244

External Source Codes: 
CAS Registry Number 606143-52-6 (see NLM ChemIDplus info)
FDA UNII Code 6UH91I579U
PDQ Closed Trial Search ID 532294
PDQ Open Trial Search ID 532294 (check for NCI PDQ open clinical trial info)
UMLS CUI C1832054

Other Properties:
     Name Value (qualifiers indented underneath)
Chemical_Formula C17H15BrClFN4O3
code C66939
Contributing_Source CTRP
Contributing_Source FDA
Legacy_Concept_Name AZD6244
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  


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