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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

Manufacturer:  MilliporeSigma™ 5.04981.0001

Catalog No. 50-498-10001


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Description

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

Specifications

99% by HPLC
Protect from Light
TrkA
DMSO
White solid
10mg
C23H21ClN6O2
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