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Dual DDR1 and DDR2 inhibitor 5n

Chemical Structure : Dual DDR1 and DDR2 inhibitor 5n

CAS No.: 2241813-33-0

Dual DDR1 and DDR2 inhibitor 5n (DDR1/2-IN-5n)

Catalog No.: PC-35543Not For Human Use, Lab Use Only.

Dual DDR1 and DDR2 inhibitor 5n is a highly potent, selective, dual Discoidin domain receptor DDR1 and DDR2 inhibitor with Kd of 7.9 and 8.0 nM, IC50 of 9.4 and 20.4 nM, repectively.

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

    Biological Activity

    Dual DDR1 and DDR2 inhibitor 5n is a highly potent, selective, dual Discoidin domain receptor DDR1 and DDR2 inhibitor with Kd of 7.9 and 8.0 nM, IC50 of 9.4 and 20.4 nM, repectively.
    Dual DDR1 and DDR2 inhibitor 5n displays significant selectivity against a panel of 403 wild-type kinases at 1 uM (Abl1 IC50=494 nM).
    Dual DDR1 and DDR2 inhibitor 5n dose-dependently inhibited lipopolysaccharide (LPS)-induced interleukin-6 (IL-6) release in mouse primary peritoneal macrophages (MPMs), attenuates lung pathophysiologic changes in LPS-challenged mice, effectively decreases the levels of TNF-α and IL-6 both in BALF and serum.

    Physicochemical Properties

    M.Wt 560.625
    Formula C31H31F3N6O
    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-(Imidazo[1,2-a]pyrazin-3-ylethynyl)-4-isopropyl-N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)benzamide

    References

    1. Wang Z, et al. J Med Chem. 2018 Aug 3. doi: 10.1021/acs.jmedchem.8b01045.

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