产品描述
| 溶解性 | Soluble in DMSO (92 mg/ml at 25 °C), water (<1 mg/ml at 25 °C), and ethanol (<1 mg/ml at 25 °C). |
| 存贮条件 | 储存温度-20°C |
| 应用 | A MEK-1 non-ATP competitive inhibitor. |
| 产品介绍 | Selumetinib (AZD6244)是一种有效，高选择性的MEK1抑制剂，IC50为14 nM，也抑制ERK1/2磷酸化，IC50为10 nM，对p38α， MKK6， EGFR， ErbB2， ERK2， B-Raf等没有抑制作用。Phase 3。 |
| 备注 | Selumetinib (AZD6244) is a potent, highly selective MEK1 inhibitor with IC50 of 14 nM, also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc. Phase 1/2. |
| 生化机理 | Selumetinib is a non-ATP competitive inhibitor of MEK-1 (IC50 = 14 nM). This compound inactivates the phosphorylation of ERK1/2 (IC50 < 40 nM). Selumetinib has little effect on p38, c-Jun-NH2-kinase, or the MEK/ERK5 pathways. |
| 别名 | 5-[(4-溴-2-氯苯基)氨基]-4-氟-N-(2-羟基乙氧基)-1-甲基-1H-苯并咪唑-6-甲酰胺;AZD6244; Array142886; ARRY-142886; AZD-6244;AZD 6244;5-[(4-Bromo-2-chlorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide |
