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Nek2 inhibitor 3a

Chemical Structure : Nek2 inhibitor 3a

CAS No.: 2514949-36-9

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Nek2 inhibitor 3a

Catalog No.: PC-61478Not For Human Use, Lab Use Only.

Nek2 inhibitor 3a is a potent, relatively selective Nek2 inhibitor with IC50 of 82.74 nM in cell-free assays.

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

    Biological Activity

    Nek2 inhibitor 3a is a potent, relatively selective Nek2 inhibitor with IC50 of 82.74 nM in cell-free assays.
    Nek2 inhibitor 3a inhibits only 3 kinases (YSK4, FLT3-ITDD835V and FLT3-ITDF691L) against 97 kinases with >65% inhibition at 15 nM.
    Nek2 inhibitor 3a blocks NEK2-EZH2 complex formation and inhibits tumor cell proliferation.
    Nek2 inhibitor 3a efficiently attenuates GBM growth in mouse model and exhibits a synergistic effect with radiotherapy.

    Physicochemical Properties

    M.Wt 568.619
    Formula C28H27F3N6O2S
    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

    (R)-5-(7-(1-(2-(dimethylamino)ethyl)-1H-pyrazol-4-yl)imidazo[1,2-a]pyridin-3-yl)-3-(1-(2-(trifluoromethyl)phenyl)ethoxy)thiophene-2-carboxamide

    References

    1. Wang J, et al. J Clin Invest. 2017 Aug 1;127(8):3075-3089.

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