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SIAIS164018

Chemical Structure : SIAIS164018

CAS No.: 2353492-68-7

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SIAIS164018

Catalog No.: PC-27487Not For Human Use, Lab Use Only.

SIAIS164018 is a potent, Brigatinib-based PROTAC degrader of multi-kinases ALK, EGFR, FAK, PYK2, PTK6 with IC50 of 2.5 nM and 6.6 nM against ALK and ALK (G1202R), respectively, promotes the ubiquitination and degradation of ALK, EGFR, FAK, PYK2 and PTK6, induces cell cycle arrest at the G1 phase and triggers cell apoptosis.

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

    Biological Activity

    SIAIS164018 is a potent, Brigatinib-based PROTAC degrader of multi-kinases ALK, EGFR, FAK, PYK2, PTK6 with IC50 of 2.5 nM and 6.6 nM against ALK and ALK (G1202R), respectively, promotes the ubiquitination and degradation of ALK, EGFR, FAK, PYK2 and PTK6, induces cell cycle arrest at the G1 phase and triggers cell apoptosis.

    Physicochemical Properties

    M.Wt 883.34
    Formula C43H48ClN10O7P
    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

    4-((2-(4-(1-(4-((5-chloro-4-((2-(dimethylphosphoryl)phenyl)amino)pyrimidin-2-yl)amino)-3-methoxyphenyl)piperidin-4-yl)piperazin-1-yl)-2-oxoethyl)amino)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione

    References

    1. Ren C, et al. J Med Chem. 2021 Jul 8;64(13):9152-9165.

    2. Chu D, et al. Bioorg Med Chem. 2026 Mar;134:118521.

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