[CAS NO. 2097002-61-2]  Selitrectinib (LOXO-195)

LOXO-195 potently inhibits diverse activated TRK kinases in vitro. At a concerntration of 1 μM, which is approximately 1,667-fold higher than its IC50 for TRKA (0.6 nmol/L), LOXO-195 is more than 1,000-fold selective for 98% of non-TRK kinases tested (228 individual kinases). LOXO-195 demonstrates potent inhibition of cell proliferation in TRK fusion–containing KM12, CUTO-3, and MO-91 cell lines (IC50 ≤ 5 nmol/L). In contrast, LOXO-195 treatment with concentrations up to 10 μmol/L has no inhibitory effect on the growth of the 84 cell lines that did not contain a TRK fusion.