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

Neuroscience

Key Properties

• CAS Number: 1223403-58-4
• MW: 428.44
• Purity: >98%
• Formula: C₂₁H₂₂F₂N₆O₂
• SMILES: O[C@H]1CCN(C1)C(=O)Nc1cnn2ccc(nc12)N1CCC[C@@H]1c1cc(F)ccc1F
• Target: Kinase
• Solubility: Soluble in DMSO (up to 5 mg/ml)

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.
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Storage & Handling

• Storage: RT
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

LOXO-101; ARRY-470

Compound Identifiers

PubChem CID

46188928