SHP394 is an orally active, selective and allosteric inhibitor of SHP2, with an IC50 of 23 nM[1].
SHP394 inhibits Caco-2 cells proliferation with the IC50 of 297 nM[1].SHP394 exhibits antiproliferation activity against the Detroit-562 pharyngeal carcinoma cell line in vitro (IC50= 1.38 μM) [1].SHP394 decreases p-ERK with an IC50 of 18 nM KYSE520 cells[1].
SHP394 (20-80 mg/kg; oral gavage; twice daily) dose-dependent reduces tumor volume[1].SHP394 (80 mg/kg; oral gavage; twice daily) causes tumor 34% regression and reduces mouse host bodyweight after dosing for 14 days[1].
[1]. Sarver P, et al. 6-Amino-3-methylpyrimidinones as Potent, Selective, and Orally Efficacious SHP2 Inhibitors. J Med Chem. 2019 Feb 28;62(4):1793-1802.