product name Tie2 kinase inhibitor
Description: 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. Tie2 kinase inhibitor exhibited significant inhibitory effect on Tie2 auto-phosphorylation and disrupted its downstream signal transduction in a dose dependent manner in human aortic endothelial cells. In addition, Tie2 kinase inhibitor exhibits moderately suppressed the activity of Tie2 tyrosine kinase in HEL cells with IC50 of 232 nM.
References: Bioorg Med Chem Lett. 2007 Sep 1;17(17):4756-60.
439.53
Formula
C26H21N3O2S
CAS No.
948557-43-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 35 mg/mL (79.6 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
2% Cremophor EL, 2% N,N-dimethylacetamide: 30 mg/mL
Synonyms
other peoduct :
| In Vitro |
In vitro 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. Kinase Assay: Turned on an incubator shaker and adjusted temperature to 30 °C. Added 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. Added 20 μL of protein per well except for background. Added Tie2 Kinase Inhibitor, typically 1 ~ 2 μL in DMSO stocks. Added 20 μL of a mixture of gamma 33p-ATP and cold ATP (1:1 v/v) per well. Covered with transparent polyester film. Incubated at 30 °C for 2 hrs in shaker, washed five times. Read plate on TopCount or other counting instrument, and results were calculated as IC50 values using normal methods. Cell Assay: In HEL cells, Tie2 Kinase Inhibitor moderately suppressed the activity of Tie2 tyrosine kinase, with an IC50 value of 232 NM. |
|---|---|
| In Vivo | 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. |
| Animal model | MOPC-315 plasmacytoma xenograft model. |
| Formulation & Dosage | Dissolved in 5% EtOH+5%cremophor+90% water.; 50 mg/kg; i.p. injection |
| References | Bioorg Med Chem Lett. 2007 Sep 1;17(17):4756-60 |
