Biological Activity:SHP099 is a highly potent, selective and orally bioavailable small-molecule SHP2 inhibitor with IC50 0.071 μM. It stabilizes SHP2 in an auto-inhibited conformation, concurrently binds to the interface of the N-terminal SH2, C-terminal SH2, and protein tyrosine phosphatase domains, thus inhibiting SHP2 activity through an allosteric mechanism. SHP099 suppresses RAS–ERK signaling to inhibit the proliferation of receptor-tyrosine-kinase-driven human cancer cells in vitro and is efficacious in mouse tumor xenograft models. SHP099’s activity provides evidence that pharmacological inhibition of SHP2 is a viable strategy to target RTK-driven cancers and presents a new chemical tool for further interrogation of the multifaceted cellular functions of SHP2 in development, tumorigenesis, RTK-driven drug resistance and immune-checkpoint modulation.How to Use:In vitro: SHP099 was used at 10 µM in vitro and cellular assays. In vivo: SHP099 was dosed orally to mouse tumor xenograft models at 75-100 mg/Kg once per day. Reference:
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