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FHP01

Chemical Structure : FHP01

CAS No.:

FHP01 (BA103, DDX3X helicase inhibitor FHP01)

Catalog No.: PC-49243Not For Human Use, Lab Use Only.

FHP01 (BA103) is a potent, small molecule inhibitor of DDX3X helicase activity with IC50 of 0.3 uM in in vitro enzyme assays, exhibits very effective antiproliferative and killing activity against different breast cancer cell types (IC50=3.058 and 3.21 μM in MDA MB 468 and MDA MB 231, respectively).

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    Biological Activity

    FHP01 (BA103) is a potent, small molecule inhibitor of DDX3X helicase activity with IC50 of 0.3 uM in in vitro enzyme assays, exhibits very effective antiproliferative and killing activity against different breast cancer cell types (IC50=3.058 and 3.21 μM in MDA MB 468 and MDA MB 231, respectively).
    FHP01 does not inhibit the ATPase activity of DDX3X and the helicase activity of DDX1 (IC50>100 uM).
    FHP01 also inhibited WNT signaling, a key tumorigenic pathway already correlated to DDX3X functions in breast cancer model cell lines.
    FHP01 inhibits ER+/PR+ (IC50 = 12.43 and 10.62 μM in MCF7 and T47D cells, respectively) and HER2+ (IC50 = 13.46 μM in SKBR3) cells, but lower in control MCF10A cells (IC50 = 28.71 μM).
    FHP01 (45 mg/kg, i.p. injection) suppresses rowth of MDA MB 231 tumor xenografts in nude mice.

    Physicochemical Properties

    M.Wt 403.409
    Formula C20H20F3N5O
    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

    1-(4-(3-butyl-1H-pyrrol-1-yl)phenyl)-3-(2-(trifluoromethyl)phenyl)urea

    References

    1. Lisa Gherardini, et al. Cancers (Basel). 2021 Sep 27;13(19):4830.

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