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MilliporeSigma™ Calbiochem™ Tie2/Trk Dual Inhibitor
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 (IC50 = 40 an
Supplier: MilliporeSigma™ 5.04981.0001
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 (IC50 = 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 (IC50 = 3.7 and 4 nM, with respective NIH 3T3 transfectant), displaying much reduced potency against PDGFR (IC50 =1.4μM) and little or no inhibitory activity toward EGFR, FGFR, or KDR (IC50 >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 .Specifications
| White | |
| TrkA | |
| DMSO | |
| Solid |
| 99% by HPLC | |
| C23H21ClN6O2 | |
| Protect from light | |
| 10 mg |
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