Larotrectinib (LOXO-101) sulfate

Catalog No.S7960 Synonyms: ARRY-470, Larotrectinib

Larotrectinib (LOXO-101) sulfate Chemical Structure

Molecular Weight(MW): 526.51

Larotrectinib (LOXO-101) sulfate is an oral potent and selective ATP-competitive inhibitor of tropomyosin receptor kinases (TRK).

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Biological Activity

Description Larotrectinib (LOXO-101) sulfate is an oral potent and selective ATP-competitive inhibitor of tropomyosin receptor kinases (TRK).
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

Cell Research:[2]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Adult male C3H/HeJ mice
  • Formulation: Labrafac;polygly-colyzed glyceride
  • Dosages: 10-100 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (189.92 mM)
Ethanol 100 mg/mL (189.92 mM)
Water 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.

Chemical Information

Molecular Weight 526.51
Formula

C21H22F2N6O2.H2O4S

CAS No. 1223405-08-0
Storage powder
Synonyms ARRY-470, Larotrectinib

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Related Antibodies

Trk receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID