Larotrectinib

SKU: orb1301362

Description

Larotrectinib (LOXO-101) is a highly selective, orally bioavailable small molecule inhibitor targeting the TRK family of kinases with low nanomolar potency (IC50 2-20 nM). It is widely used in preclinical research to investigate TRK-driven cancers, supporting both in vitro cellular assays and in vivo tumor model studies.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1223403-58-4
• MW: 428.44
• Purity: >99.99% (May vary between batches)
• Formula: C₂₁H₂₂F₂N₆O₂
• SMILES: O[C@H]1CCN(C1)C(=O)Nc1cnn2ccc(nc12)N1CCC[C@@H]1c1cc(F)ccc1F
• Target: Apoptosis,Trk receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.33 mM);DMSO:83.33 mg/mL (194.5 mM)

Bioactivity

• Target IC50:
  Trk:2-20 nM
• In Vivo:
  In vivo, Larotrectinib (60 and 200 mg/kg) reduces tumor growth in a KM12 mouse xenograft model.
• Animal Research:
  Mice were maintained under aseptic conditions. The care and treatment of experimental animals was in accordance with institutional guidelines. 5 × 10^5 KM12 cells were injected subcutaneously into the dorsal flank area of the mice. Tumor volume was monitored by direct measurement with calipers and calculated by the formula: length × (width^2)/2. Following the establishment of tumor and when the tumor size was between 150–200 mm^2, mice were randomly selected to receive diluent, 60 mg/kg/dose or 200 mg/kg/dose of Larotrectinib(LOXO-101). LOXO-101 was administered by oral gavage once daily for 14 days. After the last dose, tissue and blood were collected at 3, 6 and 24 hours post-treatment.

Storage & Handling

• Storage: keep away from direct sunlight,keep away from moisture,store at low temperature | 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

LOXO 101, LOXO101, LOXO-101, inhibit, Inhibitor, Larotrectinib, ARRY-470, ARRY470, ARRY 470, Apoptosis, Tropomyosin related kinase receptor, Trkreceptor, Trk, Trk Receptor, Trk receptor

Compound Identifiers

PubChem CID

46188928