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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-DS-1594a
DS-1594a

Chemical Structure : DS-1594a

CAS No.: 2440018-29-9

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DS-1594a (Emilumenib, DS1594a)

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

    生物&药学活性

    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.

    物理化学性质&存储条件

    分子量 574.62
    分子式 C27H29F3N6O3S
    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 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

    参考文献

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

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