Preferred Label : MEK/RAF Molecular Glue IK-595;
NCIt synonyms : MEK-RAF Complex Inhibitor IK-595; MEK/RAF Inhibitor IK-595;
NCIt definition : An orally bioavailable mitogen-activated protein kinase kinase (MAP2K, MAPK/ERK kinase,
or MEK)/RAF molecular glue and dual kinase inhibitor, with potential antineoplastic
activity. Upon oral administration, MEK/RAF molecular glue IK-595 targets and glues
B-RAF and C-RAF protein kinases with MEK, forming stable and inactive MEK-RAF complexes.
This prevents RAF-dependent phosphorylation and activation of MEK, inhibits the activity
of MEK, thereby preventing the activation of MEK-dependent effector proteins and transcription
factors, which may result in the inhibition of growth factor-mediated cell signaling
and tumor cell proliferation. In addition, this inhibits the anti-apoptotic activity
of C-RAF, which may also inhibit tumor cell proliferation. Oncogenic mutations in
RAF plays a key role in the overactivation of the RAS-mitogen-activated protein kinase
(MAPK) pathway and drives tumor cell proliferation and survival. MEK1/2 are dual-specificity
threonine/tyrosine kinases that play key roles in the activation of the RAS/RAF/MEK/ERK
pathway that regulates cell growth. This pathway is often dysregulated in a variety
of tumor cell types. CRAF-mediated reactivation of MEK and MAPK signaling leads to
resistance to MEK inhibitors. IK-595 is able to cross the blood-brain barrier (BBB).;
Molecule name : IK-595; IK 595;
Origin ID : C207942;
concept_is_in_subset
- has_target
