4-(4-(3-(3-(Tert-Butyl)-1-(Quinolin-6-Yl)-1H-Pyrazol-5-Yl)Ureido)-3-Fluorophenoxy)-N-Methylpicolinamide

Rebastinib exhibits potent biological activity as an inhibitor of several tyrosine kinases. Its selectivity for Tie2 has been demonstrated in various preclinical studies, where it effectively blocked Tie2-mediated signaling pathways that are implicated in tumor growth and metastasis. The compound has shown sub-nanomolar potency against Tie2, with an IC50 value that exceeds the limits of standard assays at high adenosine triphosphate concentrations. Clinical trials have indicated that rebastinib can induce hematologic responses in patients with chronic myeloid leukemia, particularly those harboring resistant mutations such as T315I.

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