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CCT137690 is an orally bioavailable small molecule inhibitor that dually targets Aurora kinases (pan-Aurora, including Aurora A and Aurora B) and FMS-like tyrosine kinase 3 (FLT3). Developed by The Institute of Cancer Research (ICR), it is an imidazo[4,5-b]pyridine derivative designed to treat malignancies such as acute myeloid leukemia (AML), particularly those harboring FLT3 internal tandem duplication (FLT3-ITD) mutations. By inhibiting both Aurora and FLT3 pathways, CCT137690 induces apoptosis and cell cycle arrest in the G2/M phase. It has demonstrated the ability to overcome resistance to selective FLT3 inhibitors like MLN518 (tandutinib) in preclinical models of AML and has also shown activity in colon cancer models.
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