MilliporeSigma™ Calbiochem™ Tie2/Trk Dual Inhibitor

Description

• A cell-permeable pyrrolopyrimidinyl-phenyl urea that acts as a potent, reversible, ATP-competitive inhibitor against Tie2 and TrkA kinase activity in cell-free assays (IC 50 = 40 and 0.4 nM, respectively; [ATP] = 100μM) as well as Tie2- and TrkA-dependent tyrosine phosphorylation of cellular proteins upon ligand stimulation in cultures (IC 50 = 3.7 and 4 nM, with respective NIH 3T3 transfectant), displaying much reduced potency against PDGFR (IC 50 =1.4μM) and little or no inhibitory activity toward EGFR, FGFR, or KDR (IC 50 >10μM)
• Reported to be efficacious in suppressing rat C6 glioblastoma tumor expansion (10 to 33mg/kg/d, or 10mg/kg/12 h p.o.) in vivo .