产品描述:
LOXO-195 is an inhibitor of the receptor tyrosine kinases TrkA and TrkC (IC50s = 0.6 and G595R, TrkAG667C, TrkCG623R, and TrkCG696A (IC50s = 2, 9.8, 2.3, and 50 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 + TrkAG595R, and ΔTrkA + TrkAG667C mouse xenograft models.