606143-52-6
606143-52-6
Chemical Structure
Selumetinib
Synonym(s): AZD6244; ARRY-142886
- CAS No.: 606143-52-6
- Formula:C17H15BrClFN4O3
- Molecular Weight:457.68
IUPAC Name: 5-((4-bromo-2-chlorophenyl)amino)-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzo[d]imidazole-6-carboxamide
InChIKey: CYOHGALHFOKKQC-UHFFFAOYSA-N
SMILES: O=C(NOCCO)C1=C(NC2=CC=C(Br)C=C2Cl)C(F)=C3N=CN(C)C3=C1
Biological Activity: 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. Selumetinib can penetrate the blood brain barrier (BBB)[1][2][3][4].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Selumetinib | 99.56% | 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. Selumetinib can penetrate the blood brain barrier (BBB). | ||||||||||||||||||||
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Selumetinib (Standard) | ≥98% | Selumetinib (Standard) is the analytical standard of Selumetinib. This product is intended for research and analytical applications. 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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References
- [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 [Content Brief]
- [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. [Content Brief]
- [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. [Content Brief]
- [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. [Content Brief]
Keywords
