MI-503 (MI 503) is a highly potent and orally bioavailable small-molecule inhibitor of Menin-MLL interaction with Kd of 9.3 nM.
MI-503 effectively induces differentiation of MLL leukemia cells and and substantially increases expression of CD11b, also reduces expression of Hoxa9 and Meis1.
MI-503 induces marked anti-proliferative effects in MV4;11 cells with GI50 of 200 nM.
MI-503 blocks hematologic tumors in vivo and reduces MLL leukemia tumor burden in mouse models.
