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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Ras-K-Ras G12D inhibitor KS-58
K-Ras G12D inhibitor KS-58

Chemical Structure : K-Ras G12D inhibitor KS-58

CAS No.: 2549046-46-8

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

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    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.

    物理化学性质&存储条件

    分子量 1333.60
    分子式 C64H89FN12O14S2
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    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

    参考文献

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

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