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DW0254

Chemical Structure : DW0254

CAS No.: 2031162-89-5

DW0254 (DW-0254)

Catalog No.: PC-73367Not For Human Use, Lab Use Only.

DW0254 (DW-0254) is a small molecules capable of inhibiting RAS-related C3 botulinum toxin substrate (RAC) small GTPase activation in ALL cell lines, directly binds to the hydrophobic pocket of PDE6D (Kd=436 nM, ITC), a RAS chaperone protein.

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    Biological Activity

    DW0254 (DW-0254) is a small molecules capable of inhibiting RAS-related C3 botulinum toxin substrate (RAC) small GTPase activation in ALL cell lines, directly binds to the hydrophobic pocket of PDE6D (Kd=436 nM, ITC), a RAS chaperone protein.
    DW0254 demonstrated dose-dependent RAC inhibition, arrest of proliferation and induced apoptosis in human leukemic cell lines (RS4;11 IC50=1.5-1.8 uM), also showed promising anti-leukemic activity in RAS-mutated cells (CCRF-CEM NRAS G12D, IC50=3.3-4.2 uM).
    DW0254 disrupted the interaction between PDE6D and RAS, disturbing RAS subcellular localization.
    DW0254 demonstrated anti-leukemic activity, decreased tumor progression in a murine xenograft model.

    Physicochemical Properties

    M.Wt 416.525
    Formula C25H28N4O2
    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

    3-(5-(2-(1H-indol-3-yl)ethyl)-1,3,4-oxadiazol-2-yl)-N-(4-ethylbenzyl)-N-methylpropanamide

    References

    1. Sara Canovas Nunes, et al. Blood Cancer J. 2022 Apr 14;12(4):64.

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