Potent pan-Trk inhibitor. Displays antiproliferative effects in cellular Ba/F3 assays (IC50
values are 7, 9 and 11 nM for cells containing the fusion proteins Tel-TrkC, Tel-TrkB and Tel-TrkA, respectively). Exhibits selectivity for Trk receptors over a range of kinases, with some activity at PDGFR and c-Kit (IC50
values are 0.87 and 0.91 μ
M respectively). Orally bioavailable.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Discovery of GNF-5837, a selective TRK inhibitor with efficacy in rodent cancer tumor models.
Albaugh et al.
ACS Med.Chem.Lett., 2012;3:140