NCIt definition : An orally bioavailable small-molecule inhibitor of mitogen-activated protein kinase
kinase 1 (MAP2K1 or MEK1), with potential antineoplastic activity. Cobimetinib specifically
binds to and inhibits the catalytic activity of MEK1, resulting in inhibition of extracellular
signal-related kinase 2 (ERK2) phosphorylation and activation and decreased tumor
cell proliferation. Preclinical studies have demonstrated that this agent is effective
in inhibiting the growth of tumor cells bearing a B-RAF mutation, which has been found
to be associated with many tumor types. A threonine-tyrosine kinase and a key component
of the RAS/RAF/MEK/ERK signaling pathway that is frequently activated in human tumors,
MEK1 is required for the transmission of growth-promoting signals from numerous receptor
tyrosine kinases.;
UNII : ER29L26N1X;
InChIKey : BSMCAPRUBJMWDF-KRWDZBQOSA-N;
CAS number : 934660-93-2;
Drug name : Cotellic;
Molecule name : GDC-0973; XL 518; XL-518; GDC 0973;