Potent (IC50 = 27 nM) inhibitor of the TAM family kinase AXL.1 It displayed potent activity against the pancreatic tumor cell line PSN-1 (IC50 = 6 nM). Dubermatinib also strongly inhibited the kinases Aurora A/B, JAK2, ABL1, and CHEK1. It induced apoptosis in chronic lymphocytic leukemia (CLL) cells and acted synergistically with BTK inhibitors against CLL cells.2 It inhibited neuroblastoma cell growth and enhanced sensitivity to conventional chemotherapy.3 Dubermatinib was also active in a drug-resistant acute myeloid leukemia model4 and reduced metastasis and therapy resistance in pancreatic cancer models5.
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