retv804m

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 V804M-IN-1 (RETV804M kinase inhibitor) is a wt-RET -selective RETV804M kinase inhibitors(IC50 = 20 nM).

RET-IN-3 is a RETV804M kinase inhibitor with potential anticancer activity for the study of non-small cell lung cancer.

AD80, a multikinase inhibitor, targets RET, RAF, SRC, and S6K with significantly reduced activity on mTOR.

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-29 (Compound 8W) is a selective RET kinase inhibitor. It demonstrates inhibitory effects on BaF3 cells with the CCDC6-RETV804M mutation, with an IC50 of 0.715 μM. RET-IN-29 shows potential for research in non-small cell lung cancer (NSCLC).

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.

RET-IN-11 is a potent and selective RET inhibitor that acts on RET (IC50: 6.20 nM) and RETV804M (IC50: 18.68 nM). RET-IN-11 induces apoptosis and exhibits anti-proliferative and migratory effects in LC-2/ad cells.