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GSK1120212 (JTP-74057) strongly prevented the activities of MEK1 and MEK2 kinases rather than activities of other 98 kinases.
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GSK1120212 (JTP-74057, Trametinib)

GSK1120212 (JTP-74057, Trametinib)  Citations(5)
  • Chul Min Park, .et al. Mechanisms for DNA-damaging agent-induced inactivation of ErbB2 and ErbB3 via the ERK and p38 signaling pathways, Oncol Lett, 2018, Feb; 15(2): 1758-1762 PMID: 29434871
  • Sumi T, .et al. Trametinib downregulates survivin expression in RB1-positive KRAS-mutant lung adenocarcinoma cells, Biochem Biophys Res Commun, 2018, Jun 18;501(1):253-258 PMID: 29727601
  • Toshiyuki Sumi, .et al. Survivin knockdown induces senescence in TTF-1-expressing, KRAS-mutant lung adenocarcinomas, Int J Oncol, 2018, Jul; 53(1): 33-46 PMID: 29658609
  • Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
  • Yuki Kawasaki, .et al. Feedback control of ErbB2 via ERK-mediated phosphorylation of a conserved threonine in the juxtamembrane domain, Sci Rep, 2016, 6: 31502 PMID: 27531070
  • Product Information
    Catalog Num A11029
    M. Wt 615.4
    Formula C26H23FIN5O4
    Solubility DMSO
    Purity >98%
    Storage at -20°C 3 years Powder
    CAS No. 871700-17-3
    Synonyms GSK-1120212, GSK212, Trametinib
    SMILES Code CC1=C2C(=C(N(C1=O)C)NC3=C(C=C(C=C3)I)F)C(=O)N(C(=O)N2C4=CC(=CC=C4)NC(=O)C)C5CC5

    Biological activity
    Introduction
    GSK1120212 (JTP-74057) strongly prevented the activities of MEK1 and MEK2 kinases rather than activities of other 98 kinases.
    Targets
    MEK1 (Cell-free assay) MEK2 (Cell-free assay)
    0.92 nM1.8 nM
    Solubility
    Solubility (25C) * In vitro DMSO 100 mg/mL heating (162.49 mM)
    Water <1 mg/mL (<1 mM)
    Ethanol <1 mg/mL (<1 mM)
    In vivo 30% PEG400/0.5% Tween80/5% propylene glycol 15 mg/mL
    * <1 mg/ml means slightly soluble or insoluble.
    * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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