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TDP-665759

Chemical Structure : TDP-665759

CAS No.: 787632-66-0

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TDP-665759 (TDP665759;TDP 665759)

Catalog No.: PC-60439Not For Human Use, Lab Use Only.

TDP-665759 is a small molecule inhibitor of HDM2-p53 interaction with FP IC50 of 0.7 uM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    TDP-665759 is a small molecule inhibitor of HDM2-p53 interaction with FP IC50 of 0.7 uM.
    TDP-665759 inhibits the proliferation of wt p53-expressing cell lines with average IC50 of 0.7 uM, stabilizes p53 protein levels, upregulates p53 target genes in a DNA damage-independent manner, and induces apoptosis in HepG2 cells.
    TDP-665759 increases p21(waf1/cip1) levels in mice liver samples, synergizes the effect of doxorubicin both in culture and in an A375 xenograft model.

    Physicochemical Properties

    M.Wt 706.45
    Formula C31H34Cl2IN5O2
    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

    (3S)-4-[(1R)-1-(2-Amino-4-chlorophenyl)ethyl]-3-(4-chlorophenyl)-3,4-dihydro-7-iodo-1-[3-(4-methyl-1-piperazinyl)propyl]-1H-1,4-benzodiazepine-2,5-dione

    References

    1. Koblish HK, et al. Mol Cancer Ther. 2006 Jan;5(1):160-9.

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