retwt

RET-IN-1 is a RET kinase inhibitor with IC50 values of 1 nM for RET (WT), 7 nM for RET (V804M), and 101 nM for RET (G810R).

RET-IN-27 (compound 20p) serves as a potent inhibitor of RET, exhibiting IC50 values of 3.6 nM for RETWT, 0.1 nM for RETV804L, 2.1 nM for RETV804M, and 0.3 nM for RETM918T. This compound plays a significant role in cancer research.

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.