MI-773 TFA

MI-773 TFA is an orally active, selective MDM2-p53 interaction inhibitor with a K i of 0.88 nM for MDM2. MI-773 TFA blocks the MDM2 -TP53 interaction. MI-773 TFA potently activates p53. MI-773 TFA induces Apoptosis. MI-773 TFA causes tumor regression in xenograft models of adenoid cystic carcinoma. MI-773 TFA exhibits anticancer effects in neuroblastoma. MI-773 TFA can be used for the research of adenoid cystic carcinoma ^{[1] [2]}.

In Vivo, MI-773 (10-100 mg/kg; p.o.; daily) TFA induces dose-dependent tumor growth inhibition and regression in the UM-PDX-HACC-5 adenoid cystic carcinoma model, with 100 mg/kg mediating a 127% TGI index and 86% tumor shrinkage via p53-dependent apoptosis^[1]. MI-773 (100 mg/kg; p.o.; daily) TFA mediates significant tumor regression in the ACCx6 adenoid cystic carcinoma PDX model^[1]. MI-773 (100 mg/kg; p.o.; daily) TFA mediates significant tumor regression in the ACCx9 adenoid cystic carcinoma PDX model^[1].

References:
[1]. Warner KA, et al. Targeting MDM2 for Treatment of Adenoid Cystic Carcinoma. Clin Cancer Res. 2016;22(14):3550-3559.
[2]. Chen YL, et al. MI-773, a breaker of the MDM2/p53 axis, exhibits anticancer effects in neuroblastoma via downregulation of INSM1. Oncol Lett. 2021;22(6):838.