Larotrectinib

• Description:

  Larotrectinib (LOXO-101) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C) .

• Product Name Alternative:

  LOXO-101; ARRY-470

• UNSPSC:

  12352005

• Hazard Statement:

  H302, H315, H319, H335

• Target:

  Apoptosis; Trk Receptor

• Type:

  Reference compound

• Related Pathways:

  Apoptosis; Neuronal Signaling; Protein Tyrosine Kinase/RTK

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/LOXO-101.html

• Purity:

  99.93

• Solubility:

  DMSO : ≥ 4.6 mg/mL

• Smiles:

  O=C(N1C[C@@H](O)CC1)NC2=C3N=C(N4[C@@H](C5=CC(F)=CC=C5F)CCC4)C=CN3N=C2

• Molecular Formula:

  C21H22F2N6O2

• Molecular Weight:

  428.44

• Precautions:

  H302, H315, H319, H335

• References & Citations:

  [1]Karyn Bouhana, et al. LOXO-101, a pan TRK inhibitor, For The Treatment Of TRK-driven Cancers.|[2]Nagasubramanian R, et al. Infantile Fibrosarcoma With NTRK3-ETV6 Fusion Successfully Treated With the Tropomyosin-Related Kinase Inhibitor LOXO-101. Pediatr Blood Cancer. 2016 Aug;63 (8) :1468-70.|[3]Kathryn G, et al. Genetic Modeling and Therapeutic Targeting of ETV6-NTRK3 with Loxo-101in Acute Lymphoblastic Leukemia. Blood 2016 128:278.|[4]Doebele RC, et al. An Oncogenic NTRK Fusion in a Patient with Soft-Tissue Sarcoma with Response to the Tropomyosin-Related Kinase Inhibitor LOXO-101. Cancer Discov. 2015 Oct;5 (10) :1049-57.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Launched

• Isoform:

  TrkA; TrkB; TrkC

• Citation 01:

  Bioact Mater. 2025 Nov 20:57:531-550.|Biophys Chem. 2025 Aug 12:327:107512.|bioRxiv. 04 Nov 2021.|bioRxiv. 2024 Feb 1.|BMC Cancer. 2024 Dec 5;24 (1) :1502.|Cell Rep Med. 2023 Feb 21;4 (2) :100911.|Eur J Med Chem. 2020 Aug 30;207:112744.|J Anal Sci Technol. 2020 Jun.|Life. 2025 Jan 15;15 (1) :99.|Mol Cancer Ther. 2021 Dec;20 (12) :2446-2456.|Mol Oncol. 2023 Jan;17 (1) :37-58.|Nat Commun. 2025 Jun 16;16 (1) :5283.|Ruprecht Karls University. The Faculty of Bio Sciences. 2023 Feb 2.|Spectrochim Acta A Mol Biomol Spectrosc. 2023 Nov 5:300:122914.|Nat Nanotechnol. 2025 Feb;20 (2) :311-324.|Res Sq. 2025 Apr 14.

• CAS Number:

  [1223403-58-4]