lestaurtinib

Lestaurtinib is an orally bioavailable indolocarbazole derivative and a small molecule multi-targeted tyrosine kinase inhibitor. It potently inhibits FMS-like tyrosine kinase 3 (FLT3), Janus kinase 2 (JAK2), and Tropomyosin receptor kinase A (TrkA), as well as Aurora kinase A and B. By inhibiting FLT3 autophosphorylation, it blocks FLT3 activity and induces apoptosis in tumor cells that overexpress FLT3. Lestaurtinib has been investigated primarily for the treatment of acute myelogenous leukemia (AML), especially in patients with FLT3 mutations, but has also undergone clinical trials for pancreatic cancer, prostate cancer, polycythemia vera (JAK2 V617F positive), essential thrombocytosis, and refractory neuroblastoma. The drug was originally developed from K252a as a semisynthetic staurosporine analog[1][4][5][6][8].

Other names

lestaurtinib111358-88-4