Taletrectinib

An ROS1, TrkA, and TrkC inhibitor (IC50s = 0.207, 0.622, and 0.98 nM, respectively), selective for these kinases over TrkB (IC50 = 2.28 nM), reduces the viability of JFCR-165, JFCR-168, and MGH193-1B patient-derived ROS1-CD74 fusion protein-positive NSCLC cells from 1-10,000 nM, reduces tumor volume in Ba/F3 mouse xenograft models expressing CD74-ROS1 wild-type fusion proteins or crizotinib-resistant CD74-ROS1G2032R mutant fusion proteins from 25-100 mg/kg. SMILES: C[C@@H](N)COC1=CC=C(C2=CN=C3C=CC(N[C@H](C)C4=CC(F)=CC=C4)=NN32)C=C1. InChi Code: InChI=1S/C23H24FN5O/c1-15(25)14-30-20-8-6-17(7-9-20)21-13-26-23-11-10-22(28-29(21)23)27-16(2)18-4-3-5-19(24)12-18/h3-13,15-16H,14,25H2,1-2H3,(H,27,28)/t15-,16-/m1/s1. InChi Key: HEVHTYMYEMEBPX-HZPDHXFCSA-N