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A SHP-2 inhibitor
RMC-4550 is an inhibitor of Src homology region 2 domain-containing phosphatase 2 (SHP-2; IC50 = 1.55 nM).1 It is selective for SHP-2 over a panel of 14 additional protein phosphatases and a panel of 468 protein kinases at 10 ?M. It inhibits tumor ERK phosphorylation in a KYSE-520 human esophageal cancer xenograft model in a dose-dependent manner.
1.Koltun, E.S., Aay, N., Buckl, A., et al.RMC-4550, an allosteric inhibitor of SHP2: Synthesis, structure, and anti-tumor activityCancer Res.78(13 Suppl.)(2018)
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