MI-1481

Research use only, not for human use.

MI-1481 (MI1481) is a highly potent inhibitor of the menin-MLL1 interaction with IC50 of 3.6 nM.

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; markedly reduces cell growth of murine bone marrow cells transformed with MLL-AF9 with GI50 of 34 nM, 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); downregulates the MLL fusion protein target genes, HOXA9 and MEIS1, at 100 nMin MV4;11 human MLL leukemia cells; strongly inhibits leukemia progression in vivo.

——

——

MI1481

Chromatin/Epigenetic

HMTase

HMTase

——

——

1887178-64-4

597.661

C29H30F3N7O2S

>98% (HPLC)

——

N#CC(N1C[C@@H](OC2)CNC2=O)=CC3=C1C=CC(CN4CCC(NC5=C(C=C(CC(F)(F)F)S6)C6=NC=N5)CC4)=C3C

(S)-4methyl-1-((5-oxomorpholin-2-yl)methyl)-5-((4-((6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)methyl)-1H-indole-2-carbonitrile

(-20℃)

With Ice Pack

≥ 2 years