For research use only. Not for therapeutic Use.
Selumetinib（Cat No.:I004283）is an oral, selective inhibitor of mitogen-activated protein kinase (MEK) 1 and 2, part of the RAS/RAF/MEK/ERK signaling pathway. It is used primarily for the treatment of neurofibromatosis type 1 (NF1)-associated plexiform neurofibromas and certain cancers driven by this pathway. By inhibiting MEK, Selumetinib reduces abnormal cell growth and tumor progression. Its ability to target this key pathway makes it a valuable option for treating NF1 and other RAS-driven tumors. Selumetinib’s efficacy and manageable safety profile provide a targeted approach for patients with these challenging conditions.
| Catalog Number | I004283 |
| CAS Number | 606143-52-6 |
| Synonyms | 6-(4-bromo-2-chloroanilino)-7-fluoro-N-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide |
| Molecular Formula | C17H15BrClFN4O3 |
| Purity | 98% |
| Target | MEK1/2 |
| Target Protein | |
| Appearance | Solid |
| Storage | Dry, dark and at 2 - 8 °C for six months or -20°C for two years. |
| IC50 | IC50:12 nM (MEK) |
| IUPAC Name | 6-(4-bromo-2-chloroanilino)-7-fluoro-N-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide |
| InChI | InChI=1S/C17H15BrClFN4O3/c1-24-8-21-16-13(24)7-10(17(26)23-27-5-4-25)15(14(16)20)22-12-3-2-9(18)6-11(12)19/h2-3,6-8,22,25H,4-5H2,1H3,(H,23,26) |
| InChIKey | CYOHGALHFOKKQC-UHFFFAOYSA-N |
| SMILES | CN1C=NC2=C1C=C(C(=C2F)NC3=C(C=C(C=C3)Br)Cl)C(=O)NOCCO |
| Reference | [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]. 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]. 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. [4]. Sebolt-Leopold JS, et al. Targeting the mitogen-activated protein kinase cascade to treat cancer. Nat Rev Cancer. 2004 Dec;4(12):937-47. [5]. Dela Cruz FS, et al. A case study of an integrative genomic and experimental therapeutic approach for rare tumors: identification of vulnerabilities in a pediatric poorly differentiated carcinoma. Genome Med. 2016 Oct 31;8(1):116. [6]. Weisberg E, et al. Upregulation of IGF1R by mutant RAS in leukemia and potentiation of RAS signaling inhibitors by small-molecule inhibition of IGF1R. Clin Cancer Res. 2014 Nov 1;20(21):5483-95. |
