Selitrectinib

SKU: orb1299822

Description

Selitrectinib (LOXO-195) is a highly potent and selective next-generation TRK inhibitor, targeting TrkA and TrkC with IC50 values of 0.6 and <2.5 nM, respectively. It is a valuable research tool for studying TRK-driven cancers, demonstrating activity in both cellular assays and in vivo models of acquired resistance to first-generation TRK inhibitors.

Research Area

Signal Transduction

Key Properties

• CAS Number: 2097002-61-2
• MW: 380.42
• Purity: 99.83% (May vary between batches)
• Formula: C₂₀H₂₁FN₆O
• SMILES: [H][C@]12CCCN1c1ccn3ncc(C(=O)N[C@H](C)CCc4ncc(F)cc24)c3n1
• Target: Trk receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.26 mM);DMSO:65 mg/mL (170.86 mM)

Bioactivity

• Target IC50:
  TrkA:0.6 nM |TrkC:<2.5 nM
• In Vivo:
  Selitrectinib (≥30 mg/kg) reduces tumor growth in TrkA-dependent KM12, as well as NIH 3T3 ΔTrkA, ΔTrkA + TrkAG595R, and ΔTrkA + TrkAG667C mouse xenograft models.
• Animal Research:
  Each cell line (2–5×10e6 cells) was injected subcutaneously into female nu/nu NCr mice age 7–9 weeks and allowed to grow to ~100–200 mm3 (efficacy) or ~ 500mm3 (PK-PD) prior to randomization by tumor size and treatment with each inhibitor by oral gavage. For PK-PD analysis, animals were dosed for 3 days, followed by euthanasia, excision of tumors and collection of plasma. Phospho-TRK levels in tumor lysates were determined by ELISA assay, while plasma inhibitor levels were determined by LC-MS/MS. For efficacy analysis, animals were dosed by oral gavage, and body weight and tumor size were monitored at regular intervals.

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

Inhibitor, inhibit, LOXO195, LOXO-195, LOXO 195, Selitrectinib, Trk Receptor, Trkreceptor, Trk receptor, Trk, Tropomyosin related kinase receptor

Compound Identifiers

PubChem CID

129103609