| 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 |
| 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 | |
| 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 |
| Delete | Mapping To | Ontology | Source |
|---|---|---|---|
| There are currently no mappings for this class. | |||