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MZH29

Chemical Structure : MZH29

CAS No.: 2089590-80-5

MZH29 (MZH 29)

Catalog No.: PC-35238Not For Human Use, Lab Use Only.

MZH29 is a novel potent, selective, orally active type II FLT3 inhibitor with IC50 of 9 nM and 7 nM against FLT3-WT and FLT3-ITD, respectively.

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    Biological Activity

    MZH29 is a novel potent, selective, orally active type II FLT3 inhibitor with IC50 of 9 nM and 7 nM against FLT3-WT and FLT3-ITD, respectively.
    MZH29 shows little to no inhibition for c-Kit in a panel of 50kinases。
    MZH29 efficiently induces apoptosis and inhibits FLT3 phosphorylation in vitro, inhibited the phosphorylation of FLT3, Stat5, ERK, and c-MYC in MV4-11, MOLM-11, and NOMO-1 cells。
    MZH29 inhibits FLT3-ITD/F691L and FLT3-D835V autophosphorylation and downstream signaling more potently than AC220, overcomes drug resistance in FLT3 mutant cells。
    MZH29 caused complete tumor regression and extended survival in a mouse model of AML with less toxicity (10 mg/kg).

    Physicochemical Properties

    M.Wt 560.626
    Formula C31H33FN4O5
    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-(3-fluoro-4-((6-methoxy-7-(3-morpholinopropoxy)quinolin-4-yl)oxy)phenyl)-3-(m-tolyl)urea

    References

    1. Xu B, et al. Leukemia. 2017 Apr;31(4):913-921.

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