SHP394 is a novel, potent and orally bioavailable SHP2 inhibitor with IC50 of 23 nM. It has high lipophilic efficiency, improved potency, and enhanced pharmacokinetic properties. The overall polarity of SHP394 enabled excellent aqueous solubility (0.98 mM in pH 6.8 buffer), but low permeability (Papp(A-B) 1.02 × 10–6 cm/s), and apparent efflux (B-A/A-B = 15) in Caco-2 cells. The metabolic stability of SHP394 in both rat and mouse liver microsomes indicated low clearance (Clint = 7.9–11.1 μL/min/mg; T1/2 > 2 h) for both species.

纯度：≥98%

CAS：2055757-40-7