SHP2 inhibitor 14

SHP2 inhibitor 14 is a novel potent, selective, allosteric, orally acitve SHP2 inhibitor with IC50 of 28 nM; inhibits p-ERK in KYSE-520 cells with IC50 of 93 nM, and shows antiproliferation effect with IC50 of 0.167 uM; demonstrates acceptable stability in mouse liver microsomes (Cl = 36.8, uL/min/mg, T1/2 = 60.2 min) and is sufficiently soluble (pH = 6.8 equilibrium solubility = 0.42 mM) to enable PK pharmacokinetic evaluation; modulate MAPK signaling in vivo in mice subcutaneously implanted with the KYSE520 carcinoma cell line.

References 1. Bagdanoff JT, et al. J Med Chem. 2019 Feb 8. doi: 10.1021/acs.jmedchem.8b01725. View Related Products by Target Protein Phosphatase/PTP