Larotrectinib (LOXO-101) is a highly selective, orally bioavailable, ATP-competitive inhibitor of the TRK family of receptors—TRKA, TRKB, and TRKC—with IC50 values ranging from 2 to 20 nM. It demonstrates strong selectivity over a wide panel of 226 kinases and effectively inhibits the growth of TRK fusion-positive cancer cell lines such as CUTO-3.29, KM12, and MO-91 at sub-100 nM concentrations. In vivo, larotrectinib significantly reduces tumor growth in xenograft models, including the KM12 colorectal cancer model. Reagent grade, for research purpose.
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