Chemical Structure : MI-1481
货号: PC-35104Not For Human Use, Lab Use Only.
MI-1481 (MI1481) is a highly potent inhibitor of the menin-MLL1 interaction with IC50 of 3.6 nM, 10-fold increase in inhibitory activity over MI-463 and MI-503.
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MI-1481 (MI1481) is a highly potent inhibitor of the menin-MLL1 interaction with IC50 of 3.6 nM, 10-fold increase in inhibitory activity over MI-463 and MI-503.
MI-1481 markedly reduces cell growth of murine bone marrow cells transformed with MLL-AF9 with GI50 of 34 nM.
MI-1481 demonstrates potent on target activity in MLL leukemia cells with GI50 values of 36 nM in MV4;11 (harboring MLL-AF4 fusion protein) and 61 nM in MOLM13 (harboring MLL-AF9).
MI-1481 downregulates the MLL fusion protein target genes, HOXA9 and MEIS1, at 100 nMin MV4;11 human MLL leukemia cells.
MI-1481 strongly inhibits leukemia progression in vivo.
分子量 | 597.661 | |
分子式 | C29H30F3N7O2S | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Borkin D, et al. J Med Chem. 2018 May 23. doi: 10.1021/acs.jmedchem.8b00071.
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