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BAY-958

Chemical Structure : BAY-958

CAS No.: 1335490-39-5

BAY-958 (BAY 958;BAY958;LDC526)

Catalog No.: PC-60539Not For Human Use, Lab Use Only.

BAY-958 (BAY958, LDC526) is a potent, selective PTEFb/CDK9 inhibitor with IC50 of 5 nM against CDK9/CyclinT1.

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

    Biological Activity

    BAY-958 (BAY958, LDC526) is a potent, selective PTEFb/CDK9 inhibitor with IC50 of 5 nM against CDK9/CyclinT1.
    BAY-958 displays 52/82/291/>900/>900-fold selectivity compared to CDK2/1/4/6/7.
    BAY-958 exhibits good antiproliferative activity in vitro, for example against HeLa cells (IC50=1000 nM) and MOLM-13 cells (IC50=280 nM).
    BAY-958 displays efficient cytotoxic activity against CLL cells in vitro, decreases CLL MCL-1 protein levels and triggers apoptosis rather than inhibiting proliferation.
    BAY-958 decreases splenic human CLL numbers in xenografted NSG mice, shows significant CLL cell cytotoxicity in TCL1 transgenic mice.

    Physicochemical Properties

    M.Wt 389.405
    Formula C17H16FN5O3S
    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

    (3-((4-(4-fluoro-2-methoxyphenyl)-1,3,5-triazin-2-yl)amino)phenyl)methanesulfonamide

    References

    1. Lücking U, et al. ChemMedChem. 2017 Nov 8;12(21):1776-1793.

    2. Göthert JR, et al. Oncotarget. 2018 May 29;9(41):26353-26369.

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