GDC-0623 (G-868) 是一种有效的 ATP 非竞争性MEK1抑制剂，Ki为 0.13 nM。 产品应用： 使用GDC-0623处理HCT116细胞或含KRAS突变的HCT116细胞或SW620细胞，GDC-0623以剂量和时间依赖的方式上调凋亡前体蛋白BIM表达；GDC-0623抑制A375 (BRAFV600E)、HCT116 (KRASG13D)、COLO 205、HT-29和HCT116细胞增殖，其EC50值分别为4 nM、53 nM、11 nM、18 nM和94 nM。 Information GDC-0623 (G-868) is a potent and ATP-uncompetitiveMEK1inhibitor withKiof 0.13 nM. Phase 1. Targets MEK1 0.13 nM In vitro In a panel of mutant cancer cell lines, GDC-0623 inhibits cellular proliferation with EC50 of 4 nM, 53 nM, 11 nM, 18 nM and 94 nM for A375 (BRAFV600E), HCT116 (KRASG13D), COLO 205 (V600E), HT-29 (V600E), and HCT116 (G13D) cells, respectively. In isogenic KRAS HCT116 and mutant KRAS SW620 colon cells, GDC-0623 upregulates BIM via its loss of phosphorylation at Ser69. GDC-0623 plus ABT-263 induces a synergistic cell apoptosis. In vivo GDC-0623 (40 mg/kg, p.o.) causes potent tumor growth inhibition (TGI) in mouse MiaPaCa-2 (120%), A375 (102%) and HCT116 (115%) xenografts. Cell Research(from reference) Cell lines：A375 (BRAFV600E), HCT116 (KRASG13D), COLO 205 (V600E), HT-29 (V600E), and HCT116 (G13D) cells Incubation Time：24 hours