Larotrectinib sulfate

SKU: orb1300381

Description

Larotrectinib sulfate is a potent, orally bioavailable, and selective inhibitor of the tropomyosin receptor kinase (TRK) family. It is widely used in preclinical research to investigate TRK-driven cancers, demonstrating efficacy in both in vitro cellular assays and in vivo tumor models.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1223405-08-0
• MW: 526.51
• Purity: 99.76% (May vary between batches)
• Formula: C₂₁H₂₂F₂N₆O₂·H₂O₄S
• SMILES: OS(O)(=O)=O.O[C@H]1CCN(C1)C(=O)Nc1cnn2ccc(nc12)N1CCC[C@@H]1c1cc(F)ccc1F
• Target: Trk receptor,Apoptosis
• Solubility: DMSO:50 mg/mL (94.96 mM);Ethanol:10 mg/mL (18.99 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2.5 mg/mL (4.75 mM)

Bioactivity

• In Vivo:
  Early/sustained but not late/acute administration of ARRY-470(LOXO-101) obviously attenuates bone cancer pain and blocks the ectopic sprouting of sensory nerve fibers and the formation of neuroma-like structures in the tumor-bearing bone, but no significant inhibition for tumor growth or bone remodeling. It has very limited ability crossing of the blood-brain barrier.
• In Vitro:
  Larotrectinib is a specific kinase inhibitor with nanomolar activity against TRKA/TRKB/TRKC but no other notable kinase inhibition (1 μM). Larotrectinib hasn't the inhibitory of the proliferation of Ba/F3 cells expressing other oncogene targets (EGFR, ROS1 or ALK) 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.
• Cell Research:
  Concentrations: 10,100,1000 nM. 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 is used for western blot analysis.
• Animal Research:
  Animal Models: Adult male C3H/HeJ mice. Formulation: Labrafac; polygly-colyzed glyceride. Dosages: 10-100 mg/kg. Administration: p.o.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Apoptosis, ARRY 470, ARRY470, ARRY-470 (sulfate), LOXO-101, LOXO101, LOXO 101 Sulfate, LOXO 101, LOXO-101 (sulfate), LOXO101 Sulfate, LOXO-101 sulfate, Trk receptor, Trk Receptor, Trk, Trkreceptor, Tropomyosin related kinase receptor

Compound Identifiers

PubChem CID

67330085