Selumetinib (AZD6244) 是一种高效选择性的，非 ATP 竞争性的 MEK1/2 抑制剂， 抑制 MEK1 的 IC50 为 14 nM。Selumetinib (AZD6244) 抑制 MEK1/2 磷酸化水平。 Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC 50 of 14 nM for MEK1 . Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation. In Vitro Selumetinib (AZD6244) causes a time- and dose-dependent reduction in DNA synthesis and cell viability in primary, induces growth arrest and apoptosis associated with the inactivation of ERK in primary 2-1318 cells. Selumetinib (AZD6244) (1µM) shows anti-proliferative effects through G0/G1 arrest on H-441, H-1437 cells. Selumetinib (AZD6244) results in the growth inhibition of several cell lines containing B-Raf and Ras mutations but has no effect on a normal fibroblast cell line. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Selumetinib (AZD6244, 50 and 100 mg/kg, p.o.) decreases the growth rate of 4-1318 xenografts in a dose-dependent manner; AZD6244 when given at the dose of 50 mg/kg also significantly suppresses the growth of the 5-1318, 2-1318, 26-1004, and 29-1104 xenografts . Selumetinib (ARRY-142886, 10, 25, 50, or 100 mg/kg, p.o.) is capable of inhibiting both ERK1/2 phosphorylation and growth of HT-29 xenograft tumors in nude mice. Tumor regressions are also seen in a BxPC3 xenograft model. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid
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Selumetinib sulfate
CAS number：943332-08-9 molecular formula：C17H17BrClFN4O7S
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| Chinese alias | - | ||
| English alias | 5-((4-Bromo-2-Chlorophenyl)amino)-4-Fluoro-N-(2-Hydroxyethoxy)-1-Methyl-1H-Benzimidazole-6-Carboxamide Sulfate | 5-((4-Bromo-2-Chlorophenyl)amino)-4-Fluoro-N-(2-Hydroxyethoxy)-1-Methyl-1H-Benzimidazole-6-Carboxamide Sulphate | MS-30133 | HY-50706A | Kosel | ||
| CAS number | 943332-08-9 | molecular formula | C17H17BrClFN4O7S |
| molecular weight | 555.76 g/mol | Exact mass | ≥99% |
| PSA | 171.000 Ų | logp | - |
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