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RET Kinase Inhibitor: RPI 1

No.179(November 2018)
RPI 1  (1)


RPI 1 (1) is a cell permeable ret/ptc1 kinase inhibitor and selectively inhibits the anchorage-independent growth of NIH3T3 transformants expressing the ret/ptc1 gene (NIH3T3ptc1 cells) (IC50 = 0.97 μM).1) By the tyrosine kinase assay using epidermal growth factor receptor as a target, it has been demonstrated that the inhibitory manner is ATP-competitive. 1 also inhibits hepatocyte growth factor-induced Met tyrosine phosphorylation (Tyr1234/Tyr1235) dose-dependently.2)

ret/ptc kinase: Rearranged in transformation/papillary thyroid carcinomas kinase
MET: mesenchymal–epithelial transition factor

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