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
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GDC-0623
CAS number：1168091-68-6 molecular formula：C16H14FIN4O3
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| Chinese alias | - | ||
| English alias | 5-(2-Fluoro-4-iodophenylamino)-imidazo[15-a]pyridine-6-carboxylic acid (2-hydroxyethoxy)-amide | B1349 | NCGC00254384-01 | UNII-HW67545I4Q | GDC 0623 | 5-((2-FLUORO-4-IODOPHENYL)AMINO)-N-(2-HYDROXYETHOXY)IMIDAZO[1,5-A]PYRIDINE-6-CARBOXAMIDE | Conac H | MF | ||
| CAS number | 1168091-68-6 | molecular formula | C16H14FIN4O3 |
| molecular weight | 456.21 g/mol | Exact mass | - |
| PSA | 87.900 Ų | logp | 2.284 |
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