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编 号:F275680
分子式:C39H51FN6O5S
分子量:734.92
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生物活性:
M-525 is a first-in-class, highly potent, irreversible and covalent menin-MLL protein-protein interaction inhibitor. M-525 binds to menin with an IC50 of 3 nM and achieves low nanomolar potencies in cell growth inhibition and in suppression of MLL regulated gene expression in MLL leukemia cells. Anti-leukemia activity.

体外研究:
M-525 achieves an IC50 of 3 nM in the MV4;11 cell line and has an IC50 of 2 μM in the HL-60 cell line. M-525 (3-300 nM; 24 h) is potent and effective in suppressing the expression of MEIS1 and HOX genes in MV4;11 cells carrying the MLL-AF4 fusion and in MOLM-13 cells carrying the MLL-AF9 fusion. It demonstrates high cellular specificity over non-MLL leukemia cells.
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