alk-in-6

ALK-IN-6 is an orally bioavailable inhibitor of anaplastic lymphoma kinase (ALK, IC50s: 71 nM, 18.72 nM, and 36.81 nM for ALK wild, ALK F1196M and ALK F1174L).

CEP-28122 mesylate salt (1022958-60-6 free base) is a highly selective orally active ALK inhibitor (IC50: 1.9 nM in an enzyme-based TRF assay).

Trk-IN-7 (compound I-6) is a highly potent TRK inhibitor, with IC50 values of 0.25-10 nM for TRKA, TRKB, and TRKC, respectively. It also shows significant inhibition of EML4-ALK (IC50 <15 nM) and ALK mutations G1202R, C1156Y, R1275Q, F1174L, L1197M, and G1269A (IC50 = 5-50 nM) [1].

Zilurgisertib fumarate (INB-000928 fumarate) is a potent and selective inhibitor of Activin Receptor-Like Kinase 2 (ALK2/ACVR1). It significantly inhibits ALK2 kinase activity (IC50 = 15 nM) and downregulates BMP-6-induced SMAD1/5 phosphorylation (IC50 = 63 nM). By blocking ALK2-mediated signaling, Zilurgisertib suppresses the production of hepcidin in hepatocytes (IC50 = 20 nM), thereby modulating iron metabolism. In preclinical studies, Zilurgisertib demonstrates the potential to improve anemia in cancer-induced models by effectively increasing hemoglobin levels.