ret (wt)

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

RET-IN-23 (compound 17) is a potent, orally active inhibitor of RET, displaying IC50 values of 1.32 nM for RET-WT, 2.50 nM for RET-CCDC6, 6.54 nM for RET-V804L, 1.03 nM for RET-V804M, and 1.47 nM for RET-M918T. The compound demonstrates significant anti-tumor activity [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-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.

Pralsetinib (Blu667) (BLU-667) is a highly potent, selective RET inhibitor (IC50s: 0.4, 0.3, 0.4, 0.4, and 0.4 nM for WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion).

RET-IN-19 is a potent inhibitor of RET and exhibits anticancer effects on RET-wt (IC50: 6.8 nM) and RET V804M (IC50: 13.51 nM).RET-IN-19 can be used to study non-small cell lung cancer (NSCLC).

RET-IN-13, a quinoline-based compound, effectively inhibits the RET kinase, demonstrating IC50 values of 0.5 nM for RET (WT) and 0.9 nM for RET (V804M). It holds promise for research into tumors and intestinal diseases associated with abnormal RET activation.

RET-IN-16 is a potent, selective inhibitor of RET, exhibiting IC50 values of 3.98 nM for RET(WT), 8.42 nM for RET(M918T), 15.05 nM for RET(V804L), 7.86 nM for RET(V804M), 5.43 nM for RET-CCDC6, and 8.86 nM for RET-KIF5B, indicating its high efficacy across different RET mutations. It possesses anticancer properties.

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 (IC50s: 1 nM, 7 nM, and 101 nM for RET (WT), RET (V804M) , and RET (G810R), respectively).

RET-IN-4 is a highly effective and specific RET inhibitor that can be administered orally. It demonstrates remarkable potency, with IC50 values of 1.29 nM, 1.97 nM, and 0.99 nM for inhibiting RET variants including RET (WT), RET (V804M), and RET (M918T), respectively. Moreover, RET-IN-4 exhibits superior selectivity towards kinases JAK2 (IC50 of 4.4 nM) and FLT3 (IC50 of 30.8 nM). Additionally, RET-IN-4 possesses pronounced anticancer properties.

Pralsetinib is a selective and next-generation RET inhibitor (IC50: 0.3-0.4 nM for WT RET, RET mutants V804L, V804M, M918T, and CCDC6-RET fusion). BLU-667 is an effective and selective inhibitor of RET mutations, fusions, and predicted resistant mutants.