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DOT1L R231Q inhibitor 37

Chemical Structure : DOT1L R231Q inhibitor 37

CAS No.:

DOT1L R231Q inhibitor 37

Catalog No.: PC-22999Not For Human Use, Lab Use Only.

DOT1L R231Q inhibitor 37 is a first-in-class DOT1L R231Q inhibitor, inhibits proliferation of H460 cells expressing DOT1LR231Q with IC50 of 6.18 uM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    DOT1L R231Q inhibitor 37 is a first-in-class DOT1L R231Q inhibitor, inhibits proliferation of H460 cells expressing DOT1LR231Q with IC50 of 6.18 uM.
    DOT1L R231Q inhibitor 37 exhibits remarkably weaker inhibitory activity of DOT1LWT (IC50=2.08 uM) compare to SGC0946.
    DOT1L R231Q inhibitor 37 decreases H3K79me2 level, while H3K27me3, H3K9me2, H3K4me1 and H3K36me2 levels remained relatively unchanged.
    DOT1L R231Q inhibitor 37 inhibited colony formation in H460R231Q, H1299R231Q, H1975R231Q, and H446R231Q lung cancer cells.
    DOT1L R231Q inhibitor 37 demonstrates in vivo antitumor activity in H460WT/R231Q OE CDX model.

    Physicochemical Properties

    M.Wt 705.87
    Formula C35H51N11O5
    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-(2-((4-((((2R,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl)(3-morpholinopropyl)amino)piperidin-1-yl)methyl)-1H-benzo[d]imidazol-6-yl)pivalamide

    References

    1. Zehui Tan, et al. Acta Pharm Sin B. 2024 Aug;14(8):3605-3623.

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