Introduction：Basic information about CAS 943332-08-9|AZD-6244, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | AZD-6244 |
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| CAS Number | 943332-08-9 | Molecular Weight | 555.76000 |
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| Density | / | Boiling Point | / |
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| Molecular Formula | C17H17BrClFN4O7S | Melting Point | / |
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| MSDS | / | Flash Point | / |
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Names
| Name | 6-(4-bromo-2-chloroanilino)-7-fluoro-N-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide,sulfuric acid |
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| Synonym | More Synonyms |
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AZD-6244 BiologicalActivity
| 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. |
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| Related Catalog | Signaling Pathways >>Apoptosis >>ApoptosisResearch Areas >>CancerSignaling Pathways >>MAPK/ERK Pathway >>MEK |
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| 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]. |
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| 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]. |
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| References | [1]. [1].Huynh H, et al, Targeted inhibition of the extracellular signal-regulated kinase kinase pathway with AZD6244 (ARRY-142886) in the treatment of hepatocellular carcinoma. Mol Cancer Therapy, 2007, 6 (1), 138-146 [2]. [2].Garon EB, et al. Identification of common predictive markers of in vitro response to the Mek inhibitor selumetinib (AZD6244; ARRY-142886) in human breast cancer and non-small cell lung cancer cell lines. Mol Cancer Thera, 2010, 9 (7), 1985-1994. [3]. [3].Yeh TC, et al. Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitor. Clin Cancer Res, 2007, 13 (5), 1576-1583. |
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Chemical & Physical Properties
| Molecular Formula | C17H17BrClFN4O7S |
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| Molecular Weight | 555.76000 |
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| Exact Mass | 553.96700 |
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| PSA | 174.88000 |
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| LogP | 4.60140 |
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| InChIKey | GRKFGZYYYYISDX-UHFFFAOYSA-N |
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| SMILES | Cn1cnc2c(F)c(Nc3ccc(Br)cc3Cl)c(C(=O)NOCCO)cc21.O=S(=O)(O)O |
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Synonyms
| AZD6244 Hyd-Sulf |
| UNII-807ME4B7IJ |
| AZD-6244 Hyd-Sulfate |
| ARRY-886 hydrogen sulfate |
| Selumetinib sulfate |
| AZD-6244 hydrogen sulfate |
| AZD-6244 |
