LOXO-101

LOXO-101 is an inhibitor of the tropomyosin-related kinases TrkA, TrkB, and TrkC (IC50s = 2-20 nM). It is selective for TrkA, -B, and -C over a panel of 226 kinases at 1 µM. LOXO-101 inhibits the growth of CUTO-3.29, KM12, and MO-91 patient-derived cancer cell lines (IC50s = In vivo, LOXO-101 (60 and 200 mg/kg) reduces tumor growth in a KM12 mouse xenograft model.Formal Name: (3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)-1-pyrrolidinyl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxy-1-pyrrolidinecarboxamide. CAS Number: 1223403-58-4. Synonyms: ARRY-470, Larotrectinib. Molecular Formula: C21H22F2N6O2. Formula Weight: 428.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 4 mg/ml. lambdamax: 264 nm. SMILES: O=C(N1CC[C@H](O)C1)NC2=C3N(N=C2)C=CC(N4CCC[C@@H]4C5=C(F)C=CC(F)=C5)=N3. InChi Code: InChI=1S/C21H22F2N6O2/c22-13-3-4-16(23)15(10-13)18-2-1-7-28(18)19-6-9-29-20(26-19)17(11-24-29)25-21(31)27-8-5-14(30)12-27/h3-4,6,9-11,14,18,30H,1-2,5,7-8,12H2,(H,25,31)/t14-,18+/m0/s1. InChi Key: NYNZQNWKBKUAII-KBXCAEBGSA-N.