Tie2 kinase inhibitor is a potent, reversible, and ATP-binding site-targeting Tie2 inhibitor with an IC50 of 250 nM. Tie2 kinase inhibitor has a remarkable selectivity for Tie2 over p38 (IC50 = 50 μM) and a >10-fold selectivity over VEGFR2, VEGFR3 and PDGFR1β. Tie2 kinase inhibitor showed efficacy in an in vivo model of angiogenesis and a MOPC-315 plasmacytoma xenograft model. In addition to its activity as an inhibitor of Tie2 kinase, Tie2 kinase inhibitor also shows modest activity against a variety of cultured mammalian cells.
| Cell Experiment | |
|---|---|
| Cell lines | Human aortic endothelial cells (HAECs) |
| Preparation method | Treatment of HAECs with Ang1 and Tie2 inhibitors Before use, Ang1 was preincubated with anti-poly-histidine antibody (R&D Systems, Minneapolis, MN) to form dimers prior to the treatment of HAECs. Equal numbers of HAECs were grown to confluent monolayer and starved with serum-free EBM medium for 6 h. HAECs were pretreated with Tie2 inhibitors or the carrier DMSO (final concentration at 0.5%) for 1 h followed by the stimulation with dimerized Ang1 for 10 min at 37 C. The same amount of protein was loaded into each well of SDS–PAGE. |
| Concentrations | 0, 0.1, 0.3, 1µM |
| Incubation time | 1 h |
| Animal Experiment | |
|---|---|
| Animal models | Rat model of choroidal neovascularization (CNV) |
| Formulation | PBS |
| Dosages | 10 µg/µl |
| Administration | injection |
| Molecular Weight | 439.53 |
| Formula | C26H21N3O2S |
| CAS Number | 948557-43-5 |
| Solubility (25°C) | DMSO 17 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Semones M, et al. Bioorg Med Chem Lett. Pyridinylimidazole inhibitors of Tie2 kinase.
[2] Zhou BN, et al. Org Lett. The first naturally occurring Tie2 kinase inhibitor.
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