LOXO-101

• CAT Number: I000858
• CAS Number: 1223403-58-4
• Molecular Formula: C21H22F2N6O2
• Molecular Weight: 428.44
• Purity: ≥95%
• Target: TRK inhibitor
• Solubility: DMSO: ≥ 4.6 mg/mL
• Storage: Two years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
• InChI: 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
• InChIKey: NYNZQNWKBKUAII-KBXCAEBGSA-N
• SMILES: O=C(N1CC[C@@H](C1)O)NC2=C3N=C(N4CCC[C@@H]4C5=CC(F)=CC=C5F)C=CN3N=C2

LOXO-101 (CAT: I000858), also known as larotrectinib, is a selective inhibitor of tropomyosin receptor kinases (TRK) including TRKA, TRKB, and TRKC. It is used for the treatment of solid tumors harboring NTRK gene fusions, which lead to constitutive activation of TRK signaling. LOXO-101 has demonstrated remarkable efficacy in patients with NTRK fusion-positive cancers, showing high response rates and durable responses. It is an oral medication that has shown promise in various tumor types, including pediatric and adult cancers, making it a targeted therapy option for patients with NTRK fusion-positive tumors.

Reference

1:Infantile Fibrosarcoma With NTRK3-ETV6 Fusion Successfully Treated With the Tropomyosin-Related Kinase Inhibitor LOXO-101. Nagasubramanian R, Wei J, Gordon P, Rastatter JC, Cox MC, Pappo A.Pediatr Blood Cancer. 2016 Aug;63(8):1468-70. doi: 10.1002/pbc.26026. Epub 2016 Apr 19. PMID: 27093299 Free PMC Article
2:An Oncogenic NTRK Fusion in a Patient with Soft-Tissue Sarcoma with Response to the Tropomyosin-Related Kinase Inhibitor LOXO-101. Doebele RC, Davis LE, Vaishnavi A, Le AT, Estrada-Bernal A, Keysar S, Jimeno A, Varella-Garcia M, Aisner DL, Li Y, Stephens PJ, Morosini D, Tuch BB, Fernandes M, Nanda N, Low JA.Cancer Discov. 2015 Oct;5(10):1049-57. doi: 10.1158/2159-8290.CD-15-0443. Epub 2015 Jul 27. PMID: 26216294 Free PMC Article