RET-IN-31

RET-IN-31 (Compound 13) is an orally active, selective RET inhibitor with IC50 values of 1.4 nM, 1.9 nM, and 3.8 nM for RETWT, RETV804L, and RETV804M, respectively. It also inhibits hERG and Cytochrome P450, with IC50 values of 13.6 μM, 7.9 μM, 12.8 μM, 16.9 μM, 8.9 μM, and 13.0 μM for CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP3A4-M, and CYP3A4-T, respectively. RET-IN-31 exhibits anticancer properties against cancers driven by activated RET mutations and gene fusions.