SHP394 is an orally active, selective and allosteric inhibitor of SHP2, with an IC 50 of 23 nM.
性状
Solid
IC50 & Target[1][2]
IC50: 23 nM (SHP2)
体外研究(In Vitro)
SHP394 inhibits Caco-2 cells proliferation with the IC50 of 297 nM.SHP394 exhibits antiproliferation activity against the Detroit-562 pharyngeal carcinoma cell line in vitro (IC50= 1.38 μM) .SHP394 decreases p-ERK with an IC50 of 18 nM KYSE520 cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
SHP394 (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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
参考文献
[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.
溶解度数据
In Vitro: DMSO : 24 mg/mL (51.01 mM; Need ultrasonic)配制储备液