KO-947

KO-947 is a potent and selective small molecule inhibitor of extracellular signal-regulated kinases 1 and 2 (ERK1/2), which are key components of the mitogen activated protein kinase (MAPK) pathway. By inhibiting ERK1/2, KO‑947 blocks MAPK/ERK-mediated signal transduction, leading to reduced tumor cell proliferation and survival. The MAPK/ERK pathway is frequently upregulated in various cancers, including those with BRAF or RAS mutations as well as tumors resistant to BRAF and MEK inhibitors. Preclinical studies demonstrated that KO‑947 induces tumor regression in models with dysregulated MAPK signaling. It was developed for the treatment of solid tumors but clinical development was discontinued after phase I trials[1][5][6][8].

Other names

6-benzyl-3-pyridin-4-yl-2,5-dihydro-1H-pyrazolo[4,3-g]quinazolin-7-oneERK Inhibitor KO-947ERK1/2 Inhibitor KO-947