Preferred Name

MEK/Aurora Kinase Inhibitor BI 847325

ID

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C106126

code

C106126

Concept_In_Subset

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C157712

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C177537

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C157711

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C176424

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C128784

Contributing_Source

GDC

DEFINITION

An orally available dual inhibitor of mitogen-activated protein kinase kinase (MEK) and Aurora kinases, with potential antineoplastic activity. Upon oral administration, MEK/Aurora kinase inhibitor BI 847325 selectively binds to and inhibits the activity of MEK, which both prevents the activation of MEK-dependent effector proteins and inhibits growth factor-mediated cell signaling. BI 847325 also binds to and inhibits the activity of the Aurora kinases A, B and C which may disrupt the assembly of the mitotic spindle apparatus, prevent chromosome segregation, and inhibit both cellular division and proliferation in Aurora kinase-overexpressing tumor cells. Altogether, this leads to the inhibition of cell proliferation and tumor growth as well as the induction of tumor regression. MEK, a dual-specificity threonine/tyrosine kinase that plays a key role in the activation of the RAS/RAF/MEK/ERK signaling pathway, is frequently upregulated in a variety of tumor cell types. Aurora kinases are serine-threonine kinases that play essential roles in mitotic checkpoint control and are overexpressed by a wide variety of cancer cell types.

FULL_SYN

MEK/Aurora Kinase Inhibitor BI 847325

BI 847325

Is_Value_For_GDC_Property

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C1909

label

MEK/Aurora Kinase Inhibitor BI 847325

Maps_To

MEK/Aurora Kinase Inhibitor BI 847325

NCI_Drug_Dictionary_ID

698315

PDQ_Closed_Trial_Search_ID

698315

PDQ_Open_Trial_Search_ID

698315

Preferred_Name

MEK/Aurora Kinase Inhibitor BI 847325

prefixIRI

Thesaurus:C106126

prefLabel

MEK/Aurora Kinase Inhibitor BI 847325

Semantic_Type

Pharmacologic Substance

UMLS_CUI

C3827151

subClassOf

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C1404

http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C129825

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