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DS-1594a

Chemical Structure : DS-1594a

CAS No.: 2440018-29-9

DS-1594a (Emilumenib, DS1594a)

Catalog No.: PC-49859Not For Human Use, Lab Use Only.

DS-1594a (Emilumenib) is a highly potent Menin-MLL1 inhibitor with IC50 of 1.4 nM in cell-free AlphaLISA assays, displays selective growth inhibition against AML and ALL cells with MLL1-r or NPM1c.

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

    Biological Activity

    DS-1594a (Emilumenib) is a highly potent Menin-MLL1 inhibitor with IC50 of 1.4 nM in cell-free AlphaLISA assays, displays selective growth inhibition against AML and ALL cells with MLL1-r or NPM1c.
    DS-1594a could reach the target protein and inhibits endogenous Menin protein and the exogeneous HA-MLL1N1-1395 interaction at > 30 nM in a dose-dependent manner.
    DS-1594a markedly inhibited the cellular growth of leukemic cells harboring various MLL fusion proteins (MV-4–11, MOLM-13, KOPN-8) and NPM1c (OCI-AML3) with GI50 of 2.5-28.5 nM, does not inhibit leukemic cell growth (exhibiting >350-fold selectivity) without MLL1-r or NPM1c (OCI-AML5, KG-1, HL-60 and K-562).
    DS-1594a induced differentiation and loss of clonogenic potential of human MLL-AF9-evoked murine AML-like cells, inhibited Meis1, Hoxa9, Mef2c, and Pbx3 expression.
    DS-1594a (1 uM) induced differentiation and loss of CD34 + /CD38 − cells in patient-derived MLL1-r + AML cells in vitro.
    DS-1594a induced gene expression changes through Menin-MLL1 chromatin-associated complexes.
    DS-1594a (50 mg/kg) showed in vivo antitumor efficacy in a MOLM-13 xenograft model, as well as in vivo antitumor efficacy in AML-ALL PDX models.

    Physicochemical Properties

    M.Wt 574.62
    Formula C27H29F3N6O3S
    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

    (1R, 2S, 4R)-4-({[4-(5,6-dimethoxypyridazin-3-yl)phenyl]methyl}amino)-2-{methyl[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino}cyclopentan-1-ol

    References

    1. Numata M, et al. Cancer Cell Int. 2023 Feb 25;23(1):36.

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