产品描述:
ASTX029 is an ERK inhibitor (IC50 = 2.7 nM for ERK2).{62100} It is selective for ERK over a panel of 465 kinases. ASTX029 reduces phosphorylation of p90 ribosomal S6 kinase (RSK) in mutant B-RAF-expressing A375 melanoma and mutant K-Ras-expressing HCT116 colorectal cancer cells with IC50 values of 3.3 and 4 nM, respectively. It inhibits proliferation in a panel of cancer cell lines, including melanoma, colorectal, and lung cancer cells. ASTX029 reduces tumor growth in A375, Calu-6, and COLO 205 mouse xenograft models.