Preferred Label : MEK Inhibitor IMM-6-415;
NCIt synonyms : MEKi IMM-6-415;
NCIt definition : An orally bioavailable small molecule and deep cyclic inhibitor (DCI) of mitogen-activated
protein kinase kinase (MAP2K; MAPKK; MEK), with potential antineoplastic activity.
Upon oral administration, IMM-6-415 targets, binds to and inhibits the activity of
MEK, thereby inhibiting the activation of MEK-dependent effector proteins and inhibits
the proliferation of tumor cells in which RAS and/or RAF are mutated. The threonine/tyrosine
protein kinase MEK plays a key role in the RAS/RAF/MEK/ERK signaling pathway, which
is frequently upregulated in a variety of tumor cell types and regulates key cellular
activities including cell growth, proliferation, survival, differentiation and apoptosis.
Mutations in Ras and Raf may induce constitutive signal transduction and uncontrolled
MAPK signaling. As a DCI, this agent, having a short half-life, allows for pulsatile
targeted inhibition that deprives tumor cells of sustained oncogenic pathway signaling.
It may also improve tolerability.;
Molecule name : IMM-6-415; IMM 6-415;
NCI Metathesaurus CUI : CL1927033;
Origin ID : C204812;
UMLS CUI : C5908068;
Semantic type(s)
- concept_is_in_subset
- has_target
