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LSN 3213128

Chemical Structure : LSN 3213128

CAS No.: 1941211-99-9

LSN 3213128 (LSN3213128)

Catalog No.: PC-62007Not For Human Use, Lab Use Only.

LSN 3213128 is a novel potent, selective and orally-bioavailable antifolate with potent and specific inhibitory activity for AICARFT.

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    Biological Activity

    LSN 3213128 is a novel potent, selective and orally-bioavailable antifolate with potent and specific inhibitory activity for AICARFT.
    LSN 3213128 treatment results in dramatic elevation of 5-aminoimidazole 4-carboxamide ribonucleotide (ZMP) and growth inhibition in NCI-H460 and MDA-MB-231met2 cancer cell lines.
    LSN 3213128 demonstrates tumor growth inhibition in a murine based xenograft model of triple negative breast cancer (TNBC).
    Aminoimidazole-4-carboxamide ribonucleotide formyltransferase (AICARFT) is an enzyme in the purine biosynthetic pathway.

    Physicochemical Properties

    M.Wt 409.45
    Formula C17H16FN3O4S2
    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

    N-(6-Fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)-5-[(3R)-3-hydroxypyrrolidin-1-yl]thiophene-2-sulfonamide

    References

    1. Fales KR, et al. J Med Chem. 2017 Oct 26. doi: 10.1021/acs.jmedchem.7b01046.

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