Preferred Label : Carbon C 14 Selumetinib;
NCIt synonyms : [14C] Selumetinib;
NCIt definition : A radioconjugate containing the orally available selumetinib, an inhibitor of mitogen-activated
protein kinase kinase (MEK or MAPK/ERK kinase) types 1 and 2, labeled with the radioisotope
carbon C 14. Upon oral administration, selumetinib selectively inhibits MEK1/2, which
prevents the activation of MEK1/2 dependent effector proteins and transcription factors.
This leads to an inhibition of cellular proliferation in MEK1/2-overexpressing tumor
cells. MEK 1 and 2 are dual specificity kinases that are essential mediators in the
activation of the RAS/RAF/MEK/ERK pathway and are often upregulated in various cancer
cells. Selumetinib radiolabeled with carbon C-14 may be used as a radiotracer for
pharmacokinetic studies of this agent, including its absorption, distribution, metabolism
and excretion (ADME).;
NCI Metathesaurus CUI : CL454150;
Origin ID : C111763;
UMLS CUI : C3831200;
Semantic type(s)
- concept_is_in_subset
