纯度:98% by HPLC;NMR (Conforms)
分子式:C21H22F2N6O2
分子量:428.44
溶剂:DMSO (5 mg/ml)
性状:Yellow solid
存储:RT
Activity (short version):panTRK inhibitor
Function / Pharmacology:Larotrectinib is a potent (IC50’s < 11 nM) inhibitor of tropomyosin receptor kinases A, B, and C (TrkA, B, and C).1 It is >100 fold selective against a panel of 229 kinases. Larotrectinib markedly attenuated bone cancer pain and significantly blocked the formation of neuroma-like structures and the sprouting of sensory nerve fibers. Larotrectinib caused substantial tumor regression in various cancers displaying TRK gene fusions.2-4 Larotrectinib is the first tissue agnostic drug approved by the FDA.