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NMS-0963

Chemical Structure : NMS-0963

CAS No.: 2765304-82-1

NMS-0963 (NMS0963)

Catalog No.: PC-22156Not For Human Use, Lab Use Only.

NMS-0963 (NMS0963) is a potent, selective spleen tyrosine kinase (SYK) inhibitor with biochemical IC50 of 3 nM, inhibits SYK kinase activity in SYK-dependent BaF3-TEL/SYK cells with IC50 of 27 nM.

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    Biological Activity

    NMS-0963 (NMS0963) is a potent, selective spleen tyrosine kinase (SYK) inhibitor with biochemical IC50 of 3 nM, inhibits SYK kinase activity in SYK-dependent BaF3-TEL/SYK cells with IC50 of 27 nM.
    NMS-0963 displays high selectivity within a panel of tested kinases.
    NMS-0963 effectively inhibits Syk phosphorylation and downstream signaling mediators of the BCR in treated cells.
    NMS-0963 shows low nanomolar antiproliferative activity on BaF3-TEL/SYK cell lines with >200-fold selectivity versus BaF3-TEL/SYK cell lines + IL3.
    NMS-0963 shows inhibitory activity in the diffuse large B cell lymphoma (DLBCL) cell line SUDHL-6 with IC50 of 702.4 nM.
    NMS-0963 displays good pharmacokinetics properties, with linear exposure with dose and excellent oral bioavailability.

    Physicochemical Properties

    M.Wt 451.53
    Formula C23H29N7O3
    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)-N-(1-(azetidin-1-yl)propan-2-yl)-3-(2-((3,5-dimethoxyphenyl)amino)pyrimidin-4-yl)-1-methyl-1H-pyrazole-5-carboxamide

    References

    1. Giovanni Cervi, et al. Eur J Med Chem. 2024 Apr 4:270:116375.

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