GNF-5837

SKU: orb1222917

Description

GNF-5837 is a potent, selective, and orally bioavailable pan-TRK inhibitor that inhibited tumor growth in a mouse xenograft model derived from RIE cells expressing both TRKA and NGF. The properties of GNF-5837 make it a good tool for the elucidation of TRK biology in cancer and other nononcology indications.

Key Properties

• CAS Number: 1033769-28-6
• MW: 535.49
• Purity: >98% (HPLC)
• Formula: C₂₈H₂₁F₄N₅O₂
• SMILES: Cc1c(cc(cc1)NC(=O)Nc1c(ccc(c1)C(F)(F)F)F)Nc1cc2c(cc1)/C(=C/c1ccc[nH]1)/C(=O)N2
• Target: Kit| PDGFRβ| TrkA| TrkB| TrkC
• Solubility: DMSO : ≥ 32 mg/mL; 59.76 mM

Bioactivity

• In Vivo:
  Animal model: Mouse xenograft model. Dosage: 25 mg/kg, 50 mg/kg, 100 mg/kg. Administration: Oral administration; once daily; for 10 days. Result: 72 and 100% tumor regression was observed at 50 and 100 mg/kg, respectively. At 25 mg/kg, only partial tumor growth inhibition was achieved.
  Read more...
• In Vitro:
  Cell Viability Assay Cell line: GOT1 cells. Concentration: 0.1 nM, 0.5 nM, 1 nM, 5 nM, 10 nM, 50 nM, 100 nM and 500 nM Incubation time: 72 hours, 96 hours and 144 hours. Result: Cell viability assay determined a clear decrease of GOT1 cell viabilityin a time- and dose- dependent manner. Western blot analysis. Cell line: GOT1 cells. Concentration: 5 nM, 50 nM and 500 nM. Incubation time: 24 hours. Result: Significant levels of TrkA expression, faint TrkC expression and no TrkB expression. Cell Cycle Analysis Cell line: GOT1 cells. Concentration: 5 nM, 500 nM. Incubation time: 72 hours. Result: Induced G1 cell cycle arrest. Apoptosis Analysis Cell line: GOT1 cells. Concentration: 500 nM. Incubation time: 144 hours. Result: Induced apoptosis.
  Read more...

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GNF5837 | GNF-5837 | GNF 5837

Quick Database Links

Gene Symbol

Kit| PDGFRβ| TrkA| TrkB| TrkC