拉罗替尼

  • 化学数据
CAS号 1223403-58-4 货号 BCP16262
中文名 拉罗替尼
英文名 Larotrectinib
中文别名
英文别名 ARRY-470;ARRY 470;ARRY470;LOXO-101; LOXO-101; LOXO101;
分子式 C21H22F2N6O2 分子量 428.44
  • 用途
生物活性 Larotrectinib, also known as ARRY-470 and LOXO-101, is an orally bioavailable, potent, ATP-competitive inhibitor of TRKA, TRKB, and TRKC. LOXO-101 has IC50 values in the low nanomolar range for inhibition of all three TRK family members in binding and cellular assays, with 100x selectivity over other kinases, and has shown acceptable pharmaceutical properties and safety in nonclinical models. The TRK family of neurotrophin receptors, TRKA, TRKB, and TRKC (encoded by NTRK1, NTRK2, and NTRK3 genes, respectively) and their neurotrophin ligands regulate growth, differentiation and survival of neurons.
信号通路 Angiogenesis/Protein Tyrosine Kinase 
靶 点 Trk Receptor 

结构式

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