VX-680 (MK-0457, Tozasertib)Catalog No. A10981

Quick Overview

VX-680 is a potent and selective small-molecule inhibitor of the Aurora kinases.
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VX-680 (MK-0457, Tozasertib)

VX-680 (MK-0457, Tozasertib)  Citations(2)
  • Sakamoto K,et al. Recurrent 8q24 rearrangement in blastic plasmacytoid dendritic cell neoplasm: association with immunoblastoid cytomorphology, MYC expression, and drug response, Leukemia, 2018, May 23 29795241
  • W. Joost Lesterhuis,et al. Network analysis of immunotherapy-induced regressing tumours identifies novel synergistic drug combinations, Sci Rep, 2015, 5: 12298 26193793
  • Product Information
    Catalog Num A10981
    M. Wt 464.6
    Formula C23H28N8OS
    Solubility DMSO
    Purity >98%
    Storage at -20°C 3 years Powder
    CAS No. 639089-54-6
    Synonyms N/A
    Chemical Name N-[4-[4-(4-Methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]sulfanylphenyl]cyclopropanecarboxamide
    SMILES Code CC1=CC(=NN1)NC2=NC(=NC(=C2)N3CCN(CC3)C)SC4=CC=C(C=C4)NC(=O)C5CC5

    Biological activity
    VX-680 is a potent and selective small-molecule inhibitor of the Aurora kinases.
    Aurora A (Cell-free assay) Aurora C (Cell-free assay) Aurora B (Cell-free assay) FLT3 (Cell-free assay) Bcr-Abl (Cell-free assay)
    0.6 nM(Ki app)4.6 nM(Ki app)18 nM(Ki app)30 nM(Ki)30 nM(Ki)
    Solubility (25C) * In vitro DMSO 93 mg/mL (200.17 mM)
    Water <1 mg/mL (<1 mM)
    Ethanol <1 mg/mL (<1 mM)
    In vivo 30% PEG400/0.5% Tween80/5% propylene glycol 30 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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    High Purity Kinase Inhibitors on Signaling Pathways

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