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CXF-009

Chemical Structure : CXF-009

CAS No.: 2727084-00-4

CXF-009 (CXF009)

Catalog No.: PC-73227Not For Human Use, Lab Use Only.

CXF-009 is a potent, specific, dual-warhead covalent inhibitor of FGFR4 (IC50=48 nM), forms dual-warhead covalent bonds with two cysteine residues in FGFR4.

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    Biological Activity

    CXF-009 is a potent, specific, dual-warhead covalent inhibitor of FGFR4 (IC50=48 nM), forms dual-warhead covalent bonds with two cysteine residues in FGFR4.
    CXF-009 forms covalent bonds with FGFR4(C477A) and FGFR4(C552A), respectively; display weak inhibition against FGFR1-3 with IC50 of 2579 nM, 2408 nM, and 977 nM.
    CXF-009 shows inhibitory effect agaginst FGFR4 muntants FGFR4(C477A), FGFR4(C552A), and FGFR4(C477A, C552A) with IC50 of 193 nM, 602 nM, and 1528 nM, respectively.
    CXF-009 inhibited the growth of Ba/F3 cells transformed with FGFR1-4 with IC50 values of 1562 nM, 1971 nM, 777 nM, and 38 nM, respectively.
    CXF-009 is slightly more reactive to GSH than PRN1371.

    Physicochemical Properties

    M.Wt 626.718
    Formula C33H38N8O5
    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

    N-(2-((8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(3,5-dimethoxyphenyl)-7-oxo-5,6,7,8-tetrahydropyrimido[4,5-d]pyrimidin-2-yl)amino)phenyl)acrylamide

    References

    1. Xiaojuan Chen, et al. Structure-based design of a dual-warhead covalent inhibitor of FGFR4. Commun Chem. 2022;5(1):36. Published 2022 Mar 17.

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