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BJG-03-025

Chemical Structure : BJG-03-025

CAS No.: 2553213-90-2

BJG-03-025

Catalog No.: PC-72153Not For Human Use, Lab Use Only.

BJG-03-025 is a potent, highly selective FAK tyrosine kinase inhibitor with biochemical IC50 of 20.2 nM.

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

    Biological Activity

    BJG-03-025 is a potent, highly selective FAK tyrosine kinase inhibitor with biochemical IC50 of 20.2 nM.
    BJG-03-025 demonstrates excellent kinome selectivity was profiled by KINOMEscan screening, PLK1 proved to be a false positive with IC50 of 8.3 uM, 100-300-fold selective for FAK.
    BJG-03-025 displays antiproliferative activity in three-dimensional (3D)-breast and gastric cancer models and impacts cellular signaling and migration.
    BJG-03-025 decreased phosphorylated FAK (pFAK Y397) in gastric cancer CDH1–/–RHOAY42C/+ organoid model, decreased aberrant signaling and proliferation of gastric cancer organoids.

    Physicochemical Properties

    M.Wt 563.725
    Formula C28H37N9O2S
    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

    6-((2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)amino)-2,4,9-trimethyl-4,9-dihydro-10H-pyrimido[5,4-b]thiazolo[5,4-e][1,4]diazepin-10-one

    References

    1. Brian J Groendyke, et al. ACS Med Chem Lett. 2020 Dec 14;12(1):30-38.

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