943332-08-9
943332-08-9 structure
- Name: AZD-6244
- Chemical Name: 6-(4-bromo-2-chloroanilino)-7-fluoro-N-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide,sulfuric acid
- CAS Number: 943332-08-9
- Molecular Formula: C17H17BrClFN4O7S
- Molecular Weight: 555.76000
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2018-07-10 19:54:40
- Modify Date: 2025-08-21 18:19:17
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Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.
| Name | 6-(4-bromo-2-chloroanilino)-7-fluoro-N-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide,sulfuric acid |
|---|---|
| Synonyms |
AZD6244 Hyd-Sulf
UNII-807ME4B7IJ AZD-6244 Hyd-Sulfate ARRY-886 hydrogen sulfate Selumetinib sulfate AZD-6244 hydrogen sulfate AZD-6244 |
| Description | Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation. |
|---|---|
| Related Catalog | |
| 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[1]. Selumetinib (AZD6244) (1µM) shows anti-proliferative effects through G0/G1 arrest on H-441, H-1437 cells[2]. 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[3]. |
| 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[1]. 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[3]. |
| References |
| Molecular Formula | C17H17BrClFN4O7S |
|---|---|
| Molecular Weight | 555.76000 |
| Exact Mass | 553.96700 |
| PSA | 174.88000 |
| LogP | 4.60140 |