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Selumetinib

(Synonyms: AZD6244; ARRY-142886)
98 Cited Publications
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Based on 98 publication(s) in Google Scholar

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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  • Pureté: 99.56%
  • CAS No.: 606143-52-6
  • Formule: C17H15BrClFN4O3
  • Masse moléculaire:457.68
  • Stockage:
    Powder   -20°C, 3 years , 4°C, 2 years ; In solvent   -80°C, 1 year , -20°C, 6 months
  • Selumetinib Chemical Structure
    Selumetinib Chemical Structure
  • Experimental Validation Results for Selumetinib
  • Experimental Validation Results for Selumetinib
  • Experimental Validation Results for Selumetinib
  • Experimental Validation Results for Selumetinib
  • Experimental Validation Results for Selumetinib
  • Experimental Validation Results for Selumetinib
CAS No.: 606143-52-6
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  • Selumetinib Chemical Structure
    Selumetinib Chemical Structure
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    Selumetinib purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2020 Mar 16;37(3):387-402.e7. [Abstract]

    Customer Validation
     MCF-7 cells were seeded in 10-11 M E2 to which fulvestrant (F), dabrafenib (D), trametinib (T) or selumetinib (S) were subsequently added at 10-9, 10-6, 10-7 or 10-6 M, respectively. After 6 days, proteins were measured by immunoblotting, and phosphorylation levels (as defined by the levels of the phosphorylated form over total protein) relative to the vehicle-treated cells were set to 1.

  • 1/16

    Selumetinib purchased from MedChemExpress. Usage Cited in: Drug Des Devel Ther. 2018 Apr 19:12:911-920. [Abstract]

    Customer Validation
     Immunoblotting demonstrates that AZD6244 can effectively restore upregulation of LC3-II/I and downregulation of p62 induced by RAD001 in 786-O and A498 cells.

  • 1/16

    Selumetinib purchased from MedChemExpress. Usage Cited in: PLoS One. 2018 Jul 5;13(7):e0200014. [Abstract]

    Customer Validation
     Representative immunoblots of control and NHARAS treated with Selumetinib for 24 h.

  • 1/16

    Selumetinib purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2017 Feb;16(2):334-343. [Abstract]

    Customer Validation
     Selumetinib treatment results in decreased phosphorylation of ERK1/2. Effect of Selumetinib on the expression and phosphorylation of ERK and AKT in the gastrocnemius muscle of cancer cachexia model.

  • 1/16

    Selumetinib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Feb 28;8(9):14835-14846. [Abstract]

    Customer Validation
     MEK inhibition results in reduced ERK phosphorylation.A. Western blot analysis of SEM and KOPN8 exposed to 500 nM of MEK inhibitor or vehicle control (DMSO) for 6, 24 and 48 hours. Both cell lines almost completely lose ERK phosphorylation (p-ERK), while total ERK (t-ERK) levels remain unaffected. B. Analysis of MEK phosphorylation (p-MEK) suggests exposure to MEK162 and Selumetinib results in enhanced MEK phosphorylation in both cell lines, whereas total MEK (t-MEK) levels remain constant.

  • 1/16

    Selumetinib purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2014 Nov 1;20(21):5483-95. [Abstract]

    Customer Validation
     Effects of AZD6244 as single agents, respectively, on mediators of IGF-1R- and ERK1/ERK2-signaling pathways.Effect of AZD6244 on IGF-1R protein expression levels, and phosphorylation of Erk1/Erk2.

  • Selumetinib