ltk (tyk1)

Gilteritinib (ASP2215) is a potent inhibitor of FMS-related tyrosine kinase 3 (FLT3) and AXL tyrosine kinase receptors (IC50 = 0.29 nM and <1 nM, respectively). In preclinical studies, gilteritinib demonstrated strong antileukemic and antitumor effects. Gilteritinib is currently in several Phase 3 clinical trials for acute myeloid leukemia.

Mps1-IN-1 is a potent, selective, and ATP-competitive inhibitor of Mps1 kinase (IC50: 367 nM).

Lorlatinib (PF-6463922) is an orally available, ATP-competitive inhibitor of the receptor tyrosine kinases, anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (Ros1), with potential antineoplastic activity.

Mps1-IN-1 dihydrochloride, a potent ATP-competitive inhibitor of Mps1 kinase, exhibits an IC50 of 367 nM. It effectively inhibits the activity of Mps1 mitotic kinase and disrupts spindle assembly checkpoint (SAC) function, thereby reducing the viability of both cancerous and 'normal' cells.