MI-538 is a potent and selective MLL inhibitor (Mixed Lineage Leukemia inhibitor). MI-538 demonstrated a pronounced effect in a mouse model of MLL leukemia. MI-538 displayed strong in vitro inhibition of the menin–MLL interaction with IC50 = 21 nM, and the binding affinity to menin (Kd = 6.5 nM). MI-538 showed high potency in inhibiting proliferation of MLL-AF9 transformed cells (GI50 = 83 nM), demonstrating the best cellular activity observed for any menin–MLL inhibitor reported to date. References: Borkin D, Pollock JW, Kempinska K, Purohit T, Li X, Wen B, Zhao T, Miao H, Shukla S, He M, Sun D, Cierpicki T, Grembecka J. Property focused structure-based optimization of small molecule inhibitors of the protein-protein interaction between menin and Mixed Lineage Leukemia (MLL). J Med Chem. 2016 Jan 8. [Epub head of print] PubMed PMID: 26744767.

纯度：≥98%

CAS：1857417-10-7