ret v804m in 1

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

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).

QZ2135 (compound 20) is a PROTAC degrader that specifically targets RET and exhibits antitumor activity in vivo within a Ba F3-KIF5B-RET-G810C xenograft mouse model. The compound demonstrates degradation activity with DC50 values of 4.7 nM (WT), 17.2 nM (V804M), and 73.8 nM (G810C) when targeting KIF5B-RET. QZ2135 is composed of the target protein ligand (red part) RETligand-3, the E3 ligase ligand (blue part) Lenalidomide-F, and the PROTAC Linker (black part) 7-Iodohept-1-yne, wherein the target protein ligand combined with the linker forms the conjugate RETLigand-Linker Conjugate-1.

RET-IN-12 is a RET inhibitor capable of acting on RET(WT) (IC50: 0.3 nM) and RET(V804M) (IC50: 1 nM).

RET-IN-22 (compound 17b) is a potent, selective, and orally active inhibitor of RET, exhibiting IC50 values of 20.9 nM for wild-type RET and 18.3 nM for RET-V804M. It demonstrates a highly selective inhibition profile across a broad spectrum of kinases, with notable specificity over EGFR and VEGFR2, and is implicated in exerting anticancer effects [1].