AM-7209 is a potent and selective inhibitor of the MDM2-p53 interaction with Kd of 38 pM, and IC50 of 1.6 nM.
AM-7209 potently inhibits cell growth on-target in the tumor cell line with wild-type p53 cell with IC50 of 2 nM, exhibits >12,500-fold selectivity over those with p53-deficient cells.
AM-7209 demonstrates remarkable pharmacokinetic properties and in vivo antitumor activity in both the SJSA-1 osteosarcoma xenograft model (ED50=2.6 mg/kg QD) and the HCT-116 colorectal carcinoma xenograft model (ED50=10 mg/kg QD).
