Quick Overview

BEZ235 (NVP-BEZ235) inhibits PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes.
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BEZ235 (NVP-BEZ235, Dactolisib)

BEZ235 (NVP-BEZ235, Dactolisib)  Citations(2)
  • Tzeng SF, .et al. O-Glycosylation-mediated signaling circuit drives metastatic castration-resistant prostate cancer, FASEB J, 2018, Jun 15:fj201800687 PMID: 29906246
  • Dominik Schulz, .et al. HNSCC cells resistant to EGFR pathway inhibitors are hypermutated and sensitive to DNA damaging substances, Am J Cancer Res, 2016, 6(9): 1963-1975 PMID: 27725902
  • Product Information
    Catalog Num A10133
    M. Wt 469.6
    Formula C30H23N5O
    Solubility DMSO>7mg/mL Water<1mg/mL Ethanol<1mg/mL
    Purity >98%
    Storage at -20°C 3 years Powder
    CAS No. 915019-65-7
    Synonyms N/A
    SMILES Code CC(C)(C#N)C1=CC=C(C=C1)N2C3=C4C=C(C=CC4=NC=C3N(C2=O)C)C5=CC6=CC=CC=C6N=C5

    Biological activity
    BEZ235 (NVP-BEZ235) inhibits PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes.
    Target Value
    p110αIC50: 4nM
    p110γIC50: 5nM
    mTOR(p70S6K)IC50: 6nM
    p110δIC50: 7nM
    ATRIC50: 21nM
    p110βIC50: 75nM
    EGFR/ErbB1IC50: >8.5μM
    VEGFR1/FLT1IC50: >10μM
    FLT3IC50: >10μM
    IGF-1RIC50: >10μM
    EphB4IC50: >10μM
    RETIC50: >10μM
    Tie-2IC50: >10μM
    c-MetIC50: >10μM
    FGFR(K650E)IC50: >10μM
    FAKIC50: >10μM
    JAK2IC50: >10μM
    c-AblIC50: >10μM
    c-SrcIC50: >10μM
    PKAIC50: >10μM
    Akt1/PKBαIC50: >10μM
    PDK-1IC50: >10μM
    B-Raf(V599E)IC50: >10μM
    CDK1IC50: >10μM
    Solubility (25C) * In vitro DMSO 0.01 mg/mL (<1 mM)
    Water <1 mg/mL (<1 mM)
    Ethanol <1 mg/mL (<1 mM)
    In vivo NMP/polyethylene glycol 300 (10/90, v/v) 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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