Tie2 kinase inhibitor 1

TEK

439, 53

MOPC-315 plasmacytoma xenograft model.

Tie2 kinase inhibitor is dissolved in 5% EtOH+5%cremophor+90% water.

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 uM) and a >10-fold selectivity over VEGFR2, VEGFR3, and PDGFR1beta. [1]

Tie2 kinase activity assay, Turn on an incubator shaker and adjust temperature to 30 C. Add 20 uL 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 uL of protein per well except for background. Add Tie2 kinase inhibitor, typically 1-2 uL in DMSO stocks. Add 20 uL 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 kinase inhibitor 1 is an optimized compound of SB-203580, selective to Tie2 with IC50 of 0.25 μM, 200-fold more potent than p38.