GNE-2861

第2组PAK抑制剂（PAK4、-5和-6的IC50分别为7.5、126和36nM）；对第2组PAK的选择性优于第1组PAK（PAK1、-2和-3的IC50分别为5.42、0.97和>10μM），以及1μM时的JAK3、KHS1、MAP4K4和MINK1；抑制细胞迁移并降低0.1-50μM的MDA-MB-436和MCF-10APIK3CA细胞的细胞活力；使耐药性MCF-7/LCC2乳腺癌细胞对他莫昔芬敏感。A group 2 PAK inhibitor (IC50s = 7.5, 126, and 36 nM for PAK4, -5, and -6, respectively); selective for group 2 PAKs over group 1 PAKs (IC50s = 5.42, 0.97, and >10 μM for PAK1, -2, and -3, respectively), as well as JAK3, KHS1, MAP4K4, and MINK1 at 1 μM; inhibits cell migration and reduces cell viability of MDA-MB-436 and MCF-10A PIK3CA cells from 0.1-50 μM; sensitizes drug-resistant MCF-7/LCC2 breast cancer cells to tamoxifen.