Larotrectinib sulfate (LOXO-101, ARRY-470)是一种可口服的、选择性的、ATP竞争性的原肌球蛋白受体激酶TRK的有效抑制剂。Larotrectinib 对TRKs的抑制作用可诱导细胞凋亡和G1细胞周期阻滞。 Information Larotrectinib (LOXO-101) sulfate Larotrectinib sulfate (LOXO-101, ARRY-470) is an oral potent and selective ATP-competitive inhibitor of tropomyosin receptor kinases (TRK) . Larotrectinib inhibition of TRKs induces cellular apoptosis and G1 cell-cycle arrest. Targets TRK In vitro ARRY-470(LOXO-101) is a selective kinase inhibitor with nanomolar activity against TRKA, TRKB and TRKC but no other notable kinase inhibition below 1,000 nM. ARRY-470 does not inhibit proliferation of Ba/F3 cells expressing other oncogene targets (epidermal growth factor receptor (EGFR), ALK or ROS1) or of lung and colorectal cell lines that do not harbor an NTRK1 fusion. It induces cell-cycle arrest in G1 and apoptosis of KM12 cells. In vivo Early/sustained but not late/acute administration of ARRY-470(LOXO-101) markedly attenuates bone cancer pain and significantly blocks the ectopic sprouting of sensory nerve fibers and the formation of neuroma-like structures in the tumor bearing bone, but does not have a significant effect on tumor growth or bone remodeling. It has very limited ability crossing of the blood brain barrier. Cell Research(from reference) Cell lines：Ba/F3 cells Concentrations：10, 100, 1000 nM Incubation Time：5 h