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C4-180

Chemical Structure : C4-180

CAS No.:

C4-180

Catalog No.: PC-25585Not For Human Use, Lab Use Only.

C4-180 is a potent, specific small molecule pan-RALGEF (Ras-like small GTPases exchange factors) inhibitor, specifically inhbits RAL but not MAPK/AKT signaling, impairs the interaction of RALGEFs with RAS.

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    Biological Activity

    C4-180 is a potent, specific small molecule pan-RALGEF (Ras-like small GTPases exchange factors) inhibitor, specifically inhbits RAL but not MAPK/AKT signaling, impairs the interaction of RALGEFs with RAS.
    C4-180 directly binds RALGDS with KD value of 2.55 uM in MST assays.
    C4-180 acts on both RALGDS and RGL2.
    C4-180 inhibits soft agar growth of RAS driven tumor cells with IC50 of <500 nM.
    C4-180 specifically suppress RAS signaling through the RAL pathway.
    C4-180 (40mg/kg) inhibits tumor formation and metastasis in pancreatic cancer models, with no detectable toxicity.

    Physicochemical Properties

    M.Wt 436.55
    Formula C24H25FN4OS
    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

    2-(((3-fluorobenzyl)amino)methyl)-N-(3-methoxybenzyl)-5,6-dimethylthieno[2,3-d]pyrimidin-4-amine

    References

    1. Donninger H, et al. J Biol Chem. 2025 Oct 8:110809.

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