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RPI-1 is an ATP-dependent RET kinase inhibitor. It has been shown to selectively inhibit the anchorage-independent growth of NIH3T3 cells transformed by the ret/ptc1 oncogene with an IC50 value of 0.97 µM.1 In a spontaneously metastasizing lung carcinoma xenograft mouse model, daily oral treatment with RPI-1 was reported to significantly reduce spontaneous lung metastases.2
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1. Inhibition of transforming activity of the ret/ptc1 oncoprotein by a 2-
2. Inhibition of c-