Overview

  • Product name

    AZD6244, MEK1/2 inhibitor
  • Description

    Potent, selective MEK1/2 inhibitor
  • Alternative names

    • ARRY-142886
    • Selumetinib
  • Biological description

    Potent, selective, non-ATP competitive MEK1/2 inhibitor (IC50 MEK1 = 14 nM). Also inhibits ERK1/2 phosphorylation.

  • Purity

    > 99%
  • CAS Number

    606143-52-6
  • Chemical structure

    Chemical Structure

Properties

  • Chemical name

    5-[(4-Bromo-2-chlorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide

  • Molecular weight

    457.69
  • Molecular formula

    C17H15BrClFN4O3
  • PubChem identifier

    10127622
  • Storage instructions

    Shipped at room temperature. Store at -20°C.
  • Solubility overview

    Soluble in DMSO to 100 mM and ethanol 4 mM

  • Handling

    Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

    Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

  • SMILES

    CN1C=NC2=C1C=C(C(=C2F)NC3=C(C=C(C=C3)Br)Cl)C(=O)NOCCO
  • Source

    Synthetic

References

This product has been referenced in:

  • 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 Ther 9:1985-94 (2010). Read more (PubMed: 20587667) »
  • 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 13:1576-83 (2007). Read more (PubMed: 17332304) »
  • Davies BR  et al. AZD6244 (ARRY-142886), a potent inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase 1/2 kinases: mechanism of action in vivo, pharmacokinetic/pharmacodynamic relationship, and potential for combination in preclinical models. Mol Cancer Ther 6:2209-19 (2007). Read more (PubMed: 17699718) »
  • 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 Ther 6:138-46 (2007). Read more (PubMed: 17237274) »

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