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VRX-0466617

Chemical Structure : VRX-0466617

CAS No.: 926906-64-1

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VRX-0466617 (VRX 0466617;VRX0466617)

Catalog No.: PC-60200Not For Human Use, Lab Use Only.

VRX-0466617 (VRX0466617) is a potent and selective Chk2 inhibitor with Ki/IC50 of 11 nM/120 nM.

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

    Biological Activity

    VRX-0466617 (VRX0466617) is a potent and selective Chk2 inhibitor with Ki/IC50 of 11 nM/120 nM.
    VRX-0466617 shows no inhibitory effect on Chk1 (>100 uM).
    VRX-0466617 inhibits the phosphorylation of Chk2 Ser(19) and Ser(33-35), but not of Chk2 Thr(68), prevents the IR-induced Chk2-dependent degradation of Hdmx and attenuates IR-induced apoptosis.

    Physicochemical Properties

    M.Wt 462.366
    Formula C19H20BrN5O2S
    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

    5-[4-(4-Bromoanilino)anilino]-N'-(1-hydroxypropan-2-yl)-3-oxo-1,2-thiazole-4-carboximidamide

    References

    1. Carlessi L, et al. Mol Cancer Ther. 2007 Mar; 6(3):935-44.

    2. Carlessi L, et al. Biochim Biophys Acta. 2010 Oct;1803(10):1213-23.

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