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eIF4A3-IN-1q

Chemical Structure : eIF4A3-IN-1q

CAS No.: 2132392-89-1

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eIF4A3-IN-1q

Catalog No.: PC-60161Not For Human Use, Lab Use Only.

eIF4A3-IN-1q is a potent, subtype-selective, orally available eIF4A3 inhibitor with IC50 of 0.14 uM.

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

    Biological Activity

    eIF4A3-IN-1q is a potent, subtype-selective, orally available eIF4A3 inhibitor with IC50 of 0.14 uM.
    eIF4A3-IN-1q displays no activity against eIF4A1, eIF4A2, BRR2 and DHX29 (IC50>100 uM).
    eIF4A3-IN-1q upregulates SC35 1.6 kb mRNA expression by 8-fold at 3 uM and 20-fold at 10 uM, potently inhibit cell growth in HCT-116 cells (GI50=1.18 uM).
    eIF4A3-IN-1q shows antitumor efficacy and promising PK profiles in vivo, without severe body weight loss.

    Physicochemical Properties

    M.Wt 645.861
    Formula C29H21BrClF3N4O3
    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

    (S)-5-(4-(5-bromopicolinoyl)-3-(4-chlorophenyl)piperazine-1-carbonyl)-1-phenyl-3-(trifluoromethyl)pyridin-2(1H)-one

    References

    1. Mizojiri R, et al. ACS Med Chem Lett. 2017 Sep 8;8(10):1077-1082.

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