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T-3256336

Chemical Structure : T-3256336

CAS No.: 1266227-69-3

T-3256336 (T3256336;T 3256336)

Catalog No.: PC-61034Not For Human Use, Lab Use Only.

T-3256336 is a potent, selective, orally available IAP antagonist with IC50 of 1.3, 2.2 and 200 nM for cIAP-1, cIAP-2 and XIAP, respectively.

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    Biological Activity

    T-3256336 is a potent, selective, orally available IAP antagonist with IC50 of 1.3, 2.2 and 200 nM for cIAP-1, cIAP-2 and XIAP, respectively.
    T-3256336 dose dependently antagonizes XIAP and promotes the activities of caspase-3 with EC50 of 1.3 uM in cell-free assays.
    T-3256336 induces the rapid proteasomal degradation of cIAP-1 and activates TNF-α-dependent extrinsic apoptosis signaling in cultured cells.
    T-3256336 induces cIAP-1 degradation, TNF-α production and caspase activation in cancer xenograft models.

    Physicochemical Properties

    M.Wt 605.728
    Formula C31H45F2N5O5
    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

    Pyrrolo[1,2-a]pyrazine-3-carboxamide, 2-[(2S)-2-(4,4-difluorocyclohexyl)-2-[[(2S)-2-(methylamino)-1-oxopropyl]amino]acetyl]-N-[(4R)-3,4-dihydro-2H-1-benzopyran-4-yl]-7-ethoxyoctahydro-, (3S,7R,8aR)-

    References

    1. Sumi H, et al. Mol Cancer Ther. 2013 Feb;12(2):230-40.

    2. Hashimoto K, et al. J Med Chem. 2013 Feb 14;56(3):1228-46.

    3. Sumi H, et al. Biochem Biophys Res Commun. 2016 Oct 14;479(2):179-185.

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