Selumetinib
Selumetinib is an orally bioavailable noncompetitive inhibitor of MEK1/2; it primarily displays immunosuppressive and anticancer chemotherapeutic activities. In cellular and animal models of cancer, selumetinib downregulates MAPK activation and mTOR phosphorylation and upregulates caspases 3 and 7, resulting in caspase-mediated apoptosis and inhibition of tumor growth. In an animal model of graft versus host disease (GVHD), selumetinib inhibits alloreactivity through inhibition of naïve and less-differentiated T cells. Additionally, this compound decreased serum creatine phosphokinase and aspartate aminotransferase to inhibit skeletal muscle pathology and increase muscle function in an animal model of muscular dystrophy.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18971896
| Cas No. |
606143-52-6 |
|---|---|
| Purity |
≥98% |
| Formula |
C17H15BrClFN4O3 |
| Formula Wt. |
457.68 |
| IUPAC Name |
6-(4-bromo-2-chloroanilino)-7-fluoro-N-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide |
| Synonym |
AZD6244, ARRY 142886 |
| Appearance |
White to off white powder |
Paolo M, Assunta S, Antonio R, et al. Selumetinib in Advanced Non Small Cell Lung Cancer (NSCLC) Harbouring KRAS Mutation: Endless Clinical Challenge to KRAS-mutant NSCLC. Rev Recent Clin Trials. 2013 Jun;8(2):93-100. PMID: 24063423.
Muchir A, Kim YJ, Reilly SA, et al. Inhibition of extracellular signal-regulated kinase 1/2 signaling has beneficial effects on skeletal muscle in a mouse model of Emery-Dreifuss muscular dystrophy caused by lamin A/C gene mutation. Skelet Muscle. 2013 Jul 1;3(1):17. PMID: 23815988.
Shindo T, Kim TK, Benjamin CL, et al. MEK inhibitors selectively suppress alloreactivity and graft-versus-host disease in a memory stage-dependent manner. Blood. 2013 Jun 6;121(23):4617-26. PMID: 23575444.
Sabnis GJ, Kazi A, Golubeva O, et al. Effect of selumetinib on the growth of anastrozole-resistant tumors. Breast Cancer Res Treat. 2013 Apr;138(3):699-708. PMID: 23508762.
Huynh H, Soo KC, Chow PK, et al. Targeted inhibition of the extracellular signal-regulated kinase kinase pathway with AZD6244 (ARRY-142886) in the treatment of hepatocellular carcinoma. Mol Cancer Ther. 2007 Jan;6(1):138-46. PMID: 17237274.
