Larotrectinib sulfate

Larotrectinib sulfate (LOXO-101 sulfate; ARRY-470 sulfate) 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

[1223405-08-0]

Product Name Alternative

LOXO-101 (sulfate) ; ARRY-470 (sulfate)

UNSPSC

12352005

Hazard Statement

H315, H319, H320

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-sulfate.html

Concentration

10mM

Purity

99.21

Solubility

DMSO : 50 mg/mL (ultrasonic) |H2O : 2 mg/mL (ultrasonic; adjust pH to 2 with 1M HCl)

Smiles

O=S(O)(O)=O.O=C(N1CC[C@H](O)C1)NC2=C3N=C(N4[C@@H](C5=CC(F)=CC=C5F)CCC4)C=CN3N=C2

Molecular Formula

C21H24F2N6O6S

Molecular Weight

526.51

Precautions

H315, H319, H320

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.