Larotrectinib 是一种 ATP 竞争性的、口服选择性抑制剂，对原肌凝蛋白相关激酶(TRK)家族受体的三个亚型 (TRKA，B 和C) 具有纳摩尔级别的 50% 抑制浓度。

Larotrectinib is an orally administered inhibitor of the TRK kinase and is highly selective only for the TRK family of receptors(IC50s = 2-20 nM).

In vivo, Larotrectinib?(60 and 200 mg/kg) reduces tumor growth in a KM12 mouse xenograft model[1].

Mice were maintained under aseptic conditions.?The care and treatment of experimental animals was in accordance with institutional guidelines.?5 × 10^5 KM12 cells were injected subcutaneously into the dorsal flank area of the mice.?Tumor volume was monitored by direct measurement with calipers and calculated by the formula: length × (width^2)/2.?Following the establishment of tumor and when the tumor size was between 150–200 mm^2, mice were randomly selected to receive diluent, 60 mg/kg/dose or 200 mg/kg/dose of Larotrectinib(LOXO-101).?LOXO-101 was administered by oral gavage once daily for 14 days.?After the last dose, tissue and blood were collected at 3, 6 and 24 hours post-treatment[1].

1223403-58-4

C21H22F2N6O2

428.44

LOXO-101;ARRY-470

DMSO:4.6 mg/mL (10.74 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years