Medchemexpress LLC MI-538 | 1857417-10-7 | 98.0% | 566.60 | 25 MG

Supplier:  Medchemexpress LLC 25MGHY19810

MI-538 is an inhibitor of the interaction between menin and MLL fusion proteins with an IC50 of 21 nM. For research use only. We do not sell to patients.

• Inhibits the proliferation of MLL leukemia cells with a GI50 of 83 nM.
• Shows selectivity toward MLL fusion protein transformed cells, with no effect (up to 6 μM) on control cell lines HL-60 and HM-2 that do not harbor MLL translocations.
• Binds to menin with low nanomolar affinity (Kd=6.5 nM).
• Potent cellular activity due to improved binding affinity to menin and possibly increased cell membrane permeability.
• Results in strong down-regulation of Hoxa9 and Meis1 gene expression.
• In vivo, it causes an approximately 80% reduction in MV4;11 tumor volume without significant toxicity.
• Demonstrates improved exposure (AUC values), Cmax, and lowest clearance in blood plasma.
• Has a half-life of about 1.6 h and high oral bioavailability (~50%).

Catalog No. 50-004-03025