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Dual BET-Kinase inhibitor 3

Chemical Structure : Dual BET-Kinase inhibitor 3

CAS No.: 1877286-69-5

Dual BET-Kinase inhibitor 3

Catalog No.: PC-60930Not For Human Use, Lab Use Only.

Dual BET-Kinase inhibitor 3 is a potent, dual BET bromodomain-kinase inhibitor with IC50 of 34, 1.1 and 1.1 nM for BRD4 BD1, JAK2 and FLT-3, respectively.

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    Biological Activity

    Dual BET-Kinase inhibitor 3 is a potent, dual BET bromodomain-kinase inhibitor with IC50 of 34, 1.1 and 1.1 nM for BRD4 BD1, JAK2 and FLT-3, respectively.
    Dual BET-Kinase inhibitor 3 also significantly inhibits NTRK3 (IC50=5 nM), ROS1 (IC50=11 nM), PDGFRβ (IC50=16 nM) and FGFR1 (IC50=43 nM).
    Dual BET-Kinase inhibitor 3 shows equal activity against the first and second bromodomains of BRD4 and shows only slightly reduced activity against BRDT-1.
    Dual BET-Kinase inhibitor 3 inhibits cell growth of MM and AML cell lines with IC50 of <1 uM, reduces c-MYC and p-STAT3 levels and induces G1 arrest, display differential activity across cancer cell lineages.

    Physicochemical Properties

    M.Wt 527.663
    Formula C26H34FN7O2S
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    N-(3-((2-((3-fluoro-4-(4-methylpiperazin-1-yl)phenyl)amino)-5-methylpyrimidin-4-yl)amino)phenyl)-2-methylpropane-2-sulfonamide

    References

    1. Ember SW, et al. Mol Cancer Ther. 2017 Jun;16(6):1054-1067.

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