Description
A cell-permeable, reversible, ATP-competitive, and tricyclic, benzofurano-indazolo compound that acts as a potent and specific inhibitor of class III receptor tyrosine kinases (IC50 = 300 nM for c-fms, c-kit, wt-FLT3, and internal tandem duplication (ITD)-FLT3; 1 µM for PDGFRβ). Does not affect the activities of KDR, EGFR, HER2, Abl, Src, PKA, Akt, PKC, MEK, or ERK1/2 (IC50 >10 µM). Inhibits FLT-3 ligand-dependent growth of Ba/F3 cells expressing wild type FLT-3. Reported to be useful in differentiating signal transduction pathways activated by wt-FLT3 and ITD-FLT3 in Ba/F3 cells.A cell-permeable, reversible, and ATP-competitive tricyclic benzofurano-indazolo compound that acts as a potent and specific inhibitor of class III receptor tyrosine kinases (IC50 = 0.3 µM for c-fms, c-kit, wt-FLT3 and ITD-FLT3; 1.0 µM for PDGFRβ). Does not affect the activities of KDR, EGFR, HER2, Abl, Src, PKA, AKT, PKC, MEK, or ERK1/2 (IC50 ≥ 10 µM). Has been used successfully to differentiate between the signalling pathways activated by wt-FLT3 and ITD-FLT3 in Ba/F3 cells