MI-773 is a potent MDM2-p53 protein‐protein interaction (PPI) inhibitor with high binding affinity against MDM2 (K d =8.2 nM). MI-773 has antitumor activity.
In Vitro
SAR405838 (MI-77301), an analog of MI-773, displays 10 times higher binding affinity against MDM2 than MI-773 (K d =62 vs 8.2 nM). The antitumor activity of MI-77301 is more pronounced in a set of wild type p53 xenograft models than MI-773, including SJSA-1 osteosarcoma, human prostate, melanoma, colorectal tumor, LNCAP human prostate tumor and human acute lymphoblastic leukemia. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
