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MG-002

Chemical Structure : MG-002

CAS No.: 2768406-34-2

MG-002 (MG002)

Catalog No.: PC-21688Not For Human Use, Lab Use Only.

MG-002 is a potent, second-generation, orally bioavailable eIF4A RNA helicase inhibitor, potently inhibits cap-dependent mRNA translation with IC50 of 43 nM.

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    Biological Activity

    MG-002 is a potent, second-generation, orally bioavailable eIF4A RNA helicase inhibitor, potently inhibits cap-dependent mRNA translation with IC50 of 43 nM.
    MG-002 stabilizes eIF4A1-RNA complexes, preferentially inhibits mRNAs with polypurine leader regions, and is a potent inhibitor of translation in vitro and in cellula.
    MG-002 exhibits cell viability EC50 of 1-10 nM against TNBC lines (4T1, MDA-MB-231) and ER+/HER2+ breast cancer (BT474), which is more potent anti-neoplastic activity than eFT226.
    MG-002 is primarily exerting its cytotoxic effects through eIF4A1/2 engagement.
    MG-002 (0.5 mg/kg, oral) more significantly impaired mammary tumor growth compared to eFT226 in 4T1-526 tumors models, inhibited primary TNBC tumor growth through reduced cell proliferation and increased apoptosis.

    Physicochemical Properties

    M.Wt 503.51
    Formula C27H25N3O7
    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

    (5aR,6S,7R,8R,8aS)-5a-(4-cyanophenyl)-8,8a-dihydroxy-N,1,3-trimethoxy-6-phenyl-5a,7,8,8a-tetrahydro-6H-cyclopenta[4,5]furo[3,2-c]pyridine-7-carboxamide

    References

    1. Cencic R, et al. Proc Natl Acad Sci U S A. 2024 Jan 23;121(4):e2318093121.

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