Larotrectinib sulfate

Catalog No.S7960 Batch:S796004

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Technical Data

Formula

C21H22F2N6O2.H2SO4
Molecular Weight 526.51 CAS No. 1223405-08-0
Solubility (25°C)* In vitro DMSO 100 mg/mL (189.92 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Larotrectinib sulfate is an oral potent and selective ATP-competitive inhibitor of tropomyosin receptor kinases (TRK). Larotrectinib inhibition of TRKs induces cellular apoptosis and G1 cell-cycle arrest.
Targets
TRK [1]
In vitro ARRY-470(LOXO-101) is a selective kinase inhibitor with nanomolar activity against TRKA, TRKB and TRKC but no other notable kinase inhibition below 1,000 nM. ARRY-470 does not inhibit proliferation of Ba/F3 cells expressing other oncogene targets (epidermal growth factor receptor (EGFR), ALK or ROS1) or of lung and colorectal cell lines that do not harbor an NTRK1 fusion. It induces cell-cycle arrest in G1 and apoptosis of KM12 cells[2].
In vivo Early/sustained but not late/acute administration of ARRY-470(LOXO-101) markedly attenuates bone cancer pain and significantly blocks the ectopic sprouting of sensory nerve fibers and the formation of neuroma-like structures in the tumor bearing bone, but does not have a significant effect on tumor growth or bone remodeling. It has very limited ability crossing of the blood brain barrier[1].

Protocol (from reference)

Cell Assay:[2]
  • Cell lines

    Ba/F3 cells

  • Concentrations

    10, 100, 1000 nM

  • Incubation Time

    5 h

  • Method

    Ba/F3 cells expressing MPRIP-NTRK1 (RIP-TRKA) or EV were lysed after 5 h of treatment with the indicated doses of drugs (ARRY-470; G, gefitinib 1,000 nM) or DMSO control. The cell lysate are used for western bolt analysis.
Animal Study:[1]
  • Animal Models

    Adult male C3H/HeJ mice

  • Dosages

    10-100 mg/kg

  • Administration

    p.o.

Customer Product Validation

Data from [Data independently produced by , , molecular cancer therapeutics]

Data from [Data independently produced by , , Mol Cancer Ther, 2018, 17(7):1526-1539]

Data from [Data independently produced by , , Analytical Biochemistry, 2018, 545(15):78-83]

Selleck's Larotrectinib sulfate has been cited by 22 publications

Generating in vitro models of NTRK-fusion mesenchymal neoplasia as tools for investigating kinase oncogenic activation and response to targeted therapy [ Oncogenesis, 2023, 12(1):8] PubMed: 36801905
Establishment and large-scale validation of a three-dimensional tumor model on an array chip for anticancer drug evaluation [ Front Pharmacol, 2022, 13:1032975] PubMed: 36313330
JND4135, a New Type II TRK Inhibitor, Overcomes TRK xDFG and Other Mutation Resistance In Vitro and In Vivo [ Molecules, 2022, 27(19)6500] PubMed: 36235036
Influence of Tyrosine Kinase Inhibition on OATP1B3-mediated Uptake [ Mol Pharmacol, 2022, MOLPHARM-AR-2021-000287] PubMed: 35383108
NTRK1/TrkA Activation Overrides the G2/M-Checkpoint upon Irradiation [ Cancers (Basel), 2021, 13(23)6023] PubMed: 34885133
Entrectinib Induces Apoptosis and Inhibits the Epithelial-Mesenchymal Transition in Gastric Cancer with NTRK Overexpression [ Int J Mol Sci, 2021, 23(1)395] PubMed: 35008821
NTRK Fusions Can Co-Occur With H3K27M Mutations and May Define Druggable Subclones Within Diffuse Midline Gliomas [ J Neuropathol Exp Neurol, 2021, nlab016] PubMed: 33749791
TRK inhibitors block NFKB and induce NRF2 in TRK fusion-positive colon cancer [ Journal of Cancer, 2021, 12(21): 6356-6362] PubMed: None
Mechanisms of targeted therapy resistance in a pediatric glioma driven by ETV6-NTRK3 fusion [ Cold Spring Harb Mol Case Stud, 2021, 7(5)a006109] PubMed: 34429303
An Organoid Biobank of Neuroendocrine Neoplasms Enables Genotype-Phenotype Mapping [ Cell, 2020, 183(5):1420-1435.e21] PubMed: 33159857

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.