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Tie2 kinase inhibitor 948557-43-5

Product Description

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Molecular Weight:

439.53 Tie2 Kinase Inhibitor is an optimized compound of SB-203580, selective to Tie2 with IC50 of 0.25 μM, 200-fold more potent than p38.


Biological Activity


Tie2 kinase inhibitor exhibits a moderate inhibitory activity against
Tie2 tyrosine kinase. Tie2 kinase inhibitor also shows moderate cellular
activities with IC50 of 232 nM in HEL cells. Furthermore, Tie2 kinase
inhibitor has a remarkable selectivity for Tie2 over p38 (IC50=50 μM)
and a >10-fold selectivity over VEGFR2, VEGFR3, and PDGFR1β.


In a Matrigel mouse model of Angiogenesis, Tie2 kinase inhibitor, at
doses of 25 and 50 mg/kg (i.p., b.i.d), leads to a reduction of 41% and
70% of angiogenesis, respectively. In a MOPC-315 plasmacytoma xenograft
model, Tie2 kinase inhibitor treatment results in a modest dose
dependent delay in tumor growth.


Tie2 kinase activity assay


Turn on an incubator shaker and adjust temperature to 30 °C. Add 20 μL
of 3× kinase buffer (final 20 mM Tris-HCl, pH 7, 100 mM NaCl, 12 mM MgCl2,
1 mM DTT) per well to the Flashplate. Add 20 μL of protein per well
except for background. Add Tie2 kinase inhibitor, typically 1-2 μL in
DMSO stocks. Add 20 μL of a mixture of gamma 33p-ATP and cold
ATP(1:1 v/v ) per well. Cover with transparent polyester film. Incubate
at 30 °C for 2 hours in shaker, wash five times. Read plate on TopCount
or other counting instrument, results are calculated as IC50 using
normal methods.


Tie2 receptor signal transduction assay


HEL cells are cultured at between 1 and 5 × l05 mL in
RPMI-1640 medium supplemented with 2 mM glutamine and 10% FBS as a
suspension culture. Sixteen to thirty-six hours prior to an experiment,
the necessary number of cells are passaged in

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Product Categories : Protein Tyrosine Kinase > c-Met Inhibitor