Description
SHP394 is an orally active, selective and allosteric inhibitor of SHP2, with an IC 50 of 23 nMIn VitroSHP394 inhibits Caco-2 cells proliferation with the IC 50 of 297 nM. SHP394 exhibits antiproliferation activity against the Detroit-562 pharyngeal carcinoma cell line in vitro (IC 50 = 1.38 µM). SHP394 decreases p-ERK with an IC 50 of 18 nM KYSE520 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoSHP394 (20-80 mg/kg; oral gavage; twice daily) dose-dependent reduces tumor volume. SHP394 (80 mg/kg; oral gavage; twice daily) causes tumor 34% regression and reduces mouse host bodyweight after dosing for 14 days. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Six-week old female athymic NU/NU mice were inoculated subcutaneously with Detroit-562 pharyngeal carcinoma cells. Dosage: 20, 40, and 80 mg/kg Administration: Oral gavage; twice daily Result: Demonstrated a clear dose-dependent reduction in tumor volume.Form:SolidIC50& Target:IC50: 23 nM (SHP2)