ret (g810r)

Selpercatinib (LOXO-292) is a tyrosine kinase inhibitor with antineoplastic properties, displaying IC50 values of 14.0 nM for RET (WT), 24.1 nM for RET (V804M), and 530.7 nM for RET (G810R).

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).

CQ1373 is a potent RET inhibitor that demonstrates cellular activity against BaF3 cells expressing CCDC6-RET, CCDC6-RET-G810C, and CCDC6-RET-G810R, with IC50 values of 13.0, 25.7, and 28.4 nM, respectively. It shows excellent selectivity for wild-type RET and solvent front mutants G810C R, with IC50 values of 4.2, 7.1, and 32.4 nM. CQ1373 inhibits RET phosphorylation and downstream signaling through SHC. Additionally, it induces apoptosis (Apoptosis) and cell cycle arrest in BaF3 cells. CQ1373 possesses antitumor efficacy, making it a candidate for cancer research.

RET-IN-14 is a potent inhibitor of RET, capable of acting on RET (WT) (IC50 < 0.51 nM), RET (G810R) (IC50: 9.3 nM), RET (V804M) (IC50: 1.3 nM), BTK (C481S) (IC50: 9.2 nM) and BTK (C481S) (IC50 : 15 nM). RET-IN-14 exhibits potential for tumor studies.