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PITPNM3 inhibitor C8018-7840

Chemical Structure : PITPNM3 inhibitor C8018-7840

CAS No.: 893784-03-7

PITPNM3 inhibitor C8018-7840 (C8018-7840)

Catalog No.: PC-49405Not For Human Use, Lab Use Only.

PITPNM3 inhibitor C8018-7840 is a selective small molecular inhibitor of oncogenic membrane-associated phosphatidylinositol transfer protein 3 (PITPNM3) with binding KD of 500 nM, inhibits CCL18-PITPNM3 signaling mediated cell migration and invasion.

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    Biological Activity

    PITPNM3 inhibitor C8018-7840 is a selective small molecular inhibitor of oncogenic membrane-associated phosphatidylinositol transfer protein 3 (PITPNM3) with binding KD of 500 nM, inhibits CCL18-PITPNM3 signaling mediated cell migration and invasion.
    C8018-7840 inhibited PITPNM3-induced cell migration as well as invasion in a concentration-dependent manner in MDA-MB-231 and MCF-7 cells, notably decreased CCL18-PITPNM3 induced vimentin and recovered CDH1 expression.
    C8018-7840 loaded nanoparticles (NP-C8018- 7840) with its volume ratio to PEG-PLGA at 1:20, showed favorable pharmacokinetics for in vivo use.
    C8018-7840 significantly repress metastasis of breast cancer in mouse xenograft models and organoid models.

    Physicochemical Properties

    M.Wt 529.593
    Formula C30H31N3O6
    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

    1-((4-(benzo[d][1,3]dioxol-5-ylmethyl)piperazin-1-yl)methyl)-3-hydroxy-3-(2-(4-methoxyphenyl)-2-oxoethyl)indolin-2-one

    References

    1. Zihao Liu, et al. Adv Sci (Weinh). 2022 Oct 26;e2204649.

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