cobimetinib-r-enantiomer

Description: Cobimetinib R-enantiomer is the less active R-enantiomer of Cobimetinib (formerly also known as GDC-0973, RG7420 or XL-518) which is a novel, orally bioavailable, highly potent and selective small-molecule MEK1 inhibitor with IC50 of 4.2 nM. It is an orally bioavailable small-molecule inhibitor of MEK1 with potential antineoplastic activity. GDC-0973 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.

References: Cancer Res. 2012 Jan 1; 72(1):210-9; JEJNMMI Res. 2012 May 31; 2(1):22.

Related CAS : 934660-94-3 (R-enantiomer); 934662-91-6 (racemate); 934660-93-2 (free base); 1369665-02-0 (fumarate)