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MM0299 analog 13

Chemical Structure : MM0299 analog 13

CAS No.:

MM0299 analog 13

Catalog No.: PC-49755Not For Human Use, Lab Use Only.

MM0299 analog 13 (MM 0299 derivative 13) is a potent, selective, orally bioavailable, brain-penetrant inhibitor of lanosterol synthase (LSS, competition EC50=28.7 nM) with anti-proliferative activity.

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    Biological Activity

    MM0299 analog 13 (MM 0299 derivative 13) is a potent, selective, orally bioavailable, brain-penetrant inhibitor of lanosterol synthase (LSS, competition EC50=28.7 nM) with anti-proliferative activity.
    MM0299 analog 13 induced the upregulation of 24(S),25-epoxycholesterol (EPC), and maintained anti-proliferative activity in both Mut6 cells (IC50 = 0.0443 μM) and the human GSC line UTSW63 (IC50 = 0.0293 μM).
    MM0299 analog 13 was stable in plasma (>24 h) and displayed superior metabolic stability in comparison with MM0299.
    MM0299 analog 13 (20 mg/kg p.o.) induced the production of EPC in orthotopic GBM tumors but not normal mouse brain.

    Physicochemical Properties

    M.Wt 468.33
    Formula C25H19Cl2NO4
    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

    (3aR,4R,4aR,5aS,6S,6aS)-2-(4-(2-(3,5-dichlorophenyl)-2-oxoethoxy)phenyl)-4,4a,5,5a,6,6a-hexahydro-4,6-ethenocyclopropa[f]isoindole-1,3(2H,3aH)-dione

    References

    1. Thu P Nguyen, et al. Cell Chem Biol. 2023 Feb 16;30(2):214-229.e18.

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