| Name | SHP389 |
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| Description | SHP389 (SHP-389, SHP 389) is a novel potent, selective, allosteric SHP2 inhibitor with IC50 of 36 nM, shows with impressive hERG selectivity (IC50>30 uM); inhibits p-ERK in KYSE-520 cells with IC50 of 36 nM, and shows antiproliferation effect with IC50 of 0.36 uM; demonstrated a moderate-high clearance ~83% hepatic extraction) which was under predicted in vitro by rat liver microsomes (Cl= 26.1 uL/min/mg, T1/2 = 53.2 min) assuming a hepatic blood flow of 55 mL/min/kg, also showed low oral bioavailability (~2 %F). |
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| References | 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 |
| Molecular Formula | C23H29ClN8O2 |
|---|---|
| Molecular Weight | 484.989 |