Bafetinib is primarily used in the research and development of targeted cancer therapies. It functions as a dual inhibitor of Bcr-Abl and Lyn kinases, making it particularly relevant in the treatment of chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL), especially in cases resistant to other tyrosine kinase inhibitors like imatinib. Its ability to cross the blood-brain barrier also makes it a candidate for targeting central nervous system leukemia metastases. Bafetinib shows enhanced potency against certain T315I mutant forms of Bcr-Abl, which are typically resistant to first- and second-generation inhibitors. It is mainly used in preclinical studies and clinical trials to evaluate its efficacy, safety, and pharmacokinetics in hematologic malignancies.