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K-Ras G12D inhibitor KS-58

Chemical Structure : K-Ras G12D inhibitor KS-58

CAS No.: 2549046-46-8

K-Ras G12D inhibitor KS-58 (KS-58)

Catalog No.: PC-38327Not For Human Use, Lab Use Only.

K-Ras G12D inhibitor KS-58 is the first K-Ras(G12D) selective, bicyclic peptide inhibitor with binding Ki of 22 nM.

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    Biological Activity

    K-Ras G12D inhibitor KS-58 is the first K-Ras(G12D) selective, bicyclic peptide inhibitor with binding Ki of 22 nM.
    KS-58 suppressed growth of A427 cells and PANC-1 cells (human pancreas carcinoma, G12D mutant) down to 21.1% and 50.1% at 30 uM.
    KS-58 showed significantly weaker cell growth suppression activities against A549 (human lung carcinoma, G12S mutant), H1975 (human lung carcinoma, WT), MIA PaCa-2 (human pancreas carcinoma, G12C mutant), and Capan-1 (human pancreas carcinoma, G12V mutant) cells.
    KS-58 reduced the phosphorylation of ERK down to 26.0% and 57.6% at 30 uM, respectively. Biotin-KS-58 exhibited stronger binding to K-Ras(G12D) than to other Ras proteins.
    KS-58 enters cells, binds to both forms of intracellular K-Ras(G12D)GDP/GTP, and inhibits K-Ras(G12D)GDP/GTP-effector protein interactions, thus preventing downstream Ras signal pathways, such as ERK, and suppressing cell proliferation.
    KS-58 exhibits anti-cancer activity when given as an intravenous injection to mice with subcutaneous or orthotropic PANC-1 cell xenografts.

    Physicochemical Properties

    M.Wt 1333.60
    Formula C64H89FN12O14S2
    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 DMS)

    Chemical Name/SMILES

    2-((6S,9S,12S,15S,18R,21S,23aS,33S,36S,38aS)-36-((1H-indol-3-yl)methyl)-21-butyl-9-(4-fluorobenzyl)-15-heptyl-12-(hydroxymethyl)-5,8,11,14,17,20,23,28,32,35,38-undecaoxohexatriacontahydro-1H,5H-18,33-(methanothiopropanothiomethano)dipyrrolo[1,2-a:1',2'-v][1,4,7,10,13,16,19,22,25,28,31]undecaazacyclotetratriacontin-6-yl)acetic acid

    References

    1. Kotaro Sakamoto, et al. Sci Rep. 2020 Dec 10;10(1):21671.

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