Astex ERK inhibitor X (ERK inhibitor 29) is a potent, selective ERK1/2 inhibitor that inhibits ERK catalytic activity with IC50 of 3 nM.
Astex ERK inhibitor X displays excellent selectivity toward ERK1/2 against a panel of 429 kinases, only inhibits three kinases inhibited at >50% at 100 nM and 16 kinases at 1 μM.
Astex ERK inhibitor X potently inhibits ERK catalytic activity in NCI-H358 and Calu-6 cells (K-Ras mutant NSCLC) with IC50 of 11 and 15 nM, respectively.
Astex ERK inhibitor X inhibits the proliferation of a panel of KRAS-mutant NSCLC cell lines, 55% of the KRAS-mutant NSCLC cell lines with IC50 of 1-500 nM.
Astex ERK inhibitor X demonstrates in vivo anti-tumor activity in a range of KRAS-mutant NSCLC cancer models.
