Larotrectinib
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 Specifications
CAS Number
1223403-58-4
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.
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