一种 ATP 竞争性的多激酶抑制剂,对 Trk 受体酪氨酸激酶家族具有强大的活性。 Lestaurtinib 抑制 JAK2,FLT3 和 TrkA 的 IC50 分别为 0.9,3,小于 25 nM。
Lesraurtinib, also known as CEP701; KT 5555; SP 924, is an orally bioavailable indolocarbazole derivative with antineoplastic properties. Lestaurtinib inhibits autophosphorylation of FMS-like tyrosine kinase 3 (FLT3), resulting in inhibition of FLT3 activity and induction of apoptosis in tumor cells that overexpress FLT3.