AZD3463

Not available outside of the UK & Ireland.

Biochem/physiol Actions

AZD3463 is an orally available, potent receptor tyrosine kinase (RTK) inhibtor against anaplastic lymphoma kinase ALK (Ki = 0.75 nM; IC50 = 15-21 nM with 5FAM-Srctide as substrate & 30 µM ATP), insulin-like growth factor (IGF)-1 receptor (IGF1R), ROS1 (c-Ros), and Trk-A (NTRK1). AZD3463 effectively inhibits multiple crizotinib-resistant cancer growth and displays in vivo efficacy against FLT3-ITD-dependent MOLM-13 acute myeloid leukemia (AML) as well as NGP (wt ALK) & SH-SY5Y (ALK-F1174L) neuroblastoma in mice (15 mg/kg ip.).