ASTX029

ERK抑制剂（ERK2的IC50=2.7nM）；在465种激酶中对ERK具有选择性；降低突变型B-RAF表达A375黑色素瘤和突变型K-Ras表达HCT116结直肠癌细胞中的RSK磷酸化（IC50s分别为3.3和4nM）；抑制包括黑色素瘤、结直肠癌和肺癌细胞在内的一系列癌细胞系的增殖；降低A375、Calu-6和COLO 205小鼠异种移植模型中的肿瘤生长。An ERK inhibitor (IC50 = 2.7 nM for ERK2); selective for ERK over a panel of 465 kinases; reduces RSK phosphorylation in mutant B-RAF-expressing A375 melanoma and mutant K-Ras-expressing HCT116 colorectal cancer cells (IC50s = 3.3 and 4 nM, respectively); inhibits proliferation in a panel of cancer cell lines, including melanoma, colorectal, and lung cancer cells; reduces tumor growth in A375, Calu-6, and COLO 205 mouse xenograft models.分子式C29H31ClFN5O5分子量584O=C1C2=CC(C3=NC(NC4CCOCC4)=NC=C3Cl)=CC=C2CN1[C@H](C)C(N[C@@H](C5=CC(OC)=CC(F)=C5)CO)=O