Cayman LOXO-195

LOXO-195 is an inhibitor of the receptor tyrosine kinases TrkA and TrkC (IC₅₀s = 0.6 and <2.5 nM, respectively, in kinase assays). It also inhibits several Trk kinase mutants, including TrkA^G595R, TrkA^G667C, TrkC^G623R, and TrkC^G696A (IC₅₀s = 2, 9.8, 2.3, and <2.5 nM, respectively). LOXO-195 binds to the kinase domain of TrkB with an IC₅₀ value of 1.9 nM. It selectively inhibits proliferation of Trk fusion-positive K12, CUTO-3, and MO-91 cell lines (IC₅₀s = ≤5 nM) over Trk fusion-negative cell lines when used at concentrations up to 10 μM. LOXO-195 (≥30 mg/kg) reduces tumor growth in TrkA-dependent KM12, as well as NIH 3T3 ΔTrkA, ΔTrkA + TrkA^G595R, and ΔTrkA + TrkA^G667C mouse xenograft models.

WARNING This product is not for human or veterinary use.