942655-44-9
942655-44-9 structure
- Name: JK-P3
- Chemical Name: JK-P3
- CAS Number: 942655-44-9
- Molecular Formula: C18H17N3O3
- Molecular Weight: 323.35
- Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK FGFR
- Create Date: 2018-05-20 08:00:00
- Modify Date: 2024-02-28 11:08:56
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JK-P3 is a potent and pan VEGFR2 inhibitor, with IC50s of 7.83 μM, 27 μM and 5.18 μM for VEGFR2, FGFR1 and FGFR3, respectively. JK-P3 can inhibit VEGF-A-stimulated VEGFR2 activation and intracellular signalling, also inhibits endothelial monolayer wound closure and angiogenesis, as well as fibroblast growth factor receptor kinase activity in vitro. JK-P3 has anti-angiogenic activity[1].
| Name | JK-P3 |
|---|---|
| Synonyms |
Benzamide, 3,4-dimethoxy-N-(3-phenyl-1H-pyrazol-5-yl)-
3,4-Dimethoxy-N-(3-phenyl-1H-pyrazol-5-yl)benzamide |
| Description | JK-P3 is a potent and pan VEGFR2 inhibitor, with IC50s of 7.83 μM, 27 μM and 5.18 μM for VEGFR2, FGFR1 and FGFR3, respectively. JK-P3 can inhibit VEGF-A-stimulated VEGFR2 activation and intracellular signalling, also inhibits endothelial monolayer wound closure and angiogenesis, as well as fibroblast growth factor receptor kinase activity in vitro. JK-P3 has anti-angiogenic activity[1]. |
|---|---|
| Related Catalog | |
| Target |
VEGFR2:7.83 μM (IC50) FGFR1:27 μM (IC50) FGFR3:5.18 μM (IC50) |
| In Vitro | JK-P3 (0.01-10 μM; 1 hour) inhibits VEGF-A-mediated VEGFR2 phosphorylation and downstream signalling[1]. JK-P3 (0.01-10 μM; 16 hours) dose not inhibit HUVEC cell proliferation at 0.01~1 μM, and shows slight inhibitory activity at 10 μM[1]. JK-P3 (1 and 10 μM; 1 hour) does not significantly inhibit VEGF-A-stimulated endothelial tube formation at 1 µM, but almost completely inhibits the ability of endothelial cells to form into elongated hollow tubes in the presence of VEGF-A at 10 µM[1]. Western Blot Analysis Cell Line: Primary endothelial cells (treated for 7.5 min with 25 ng/mL VEGF-A)[1] Concentration: 0.01, 0.1, 1 and 10 μM Incubation Time: 1 hour Result: Almost completely inhibited VEGFR2 Y1175 phosphorylation, also inhibited VEGF-A-stimulated PLCγ1, Akt and ERK1/2 phosphorylation. Cell Proliferation Assay Cell Line: HUVEC[1] Concentration: 0.01, 0.1, 1 and 10 μM Incubation Time: 16 hours Result: Failed to inhibit endothelial cell proliferation at 0.01~1 μM but elicited a small but significant increase in cell proliferation at certain lower concentrations. |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Boiling Point | 499.6±45.0 °C at 760 mmHg |
| Molecular Formula | C18H17N3O3 |
| Molecular Weight | 323.35 |
| Flash Point | 255.9±28.7 °C |
| Exact Mass | 323.126984 |
| LogP | 3.42 |
| Vapour Pressure | 0.0±1.3 mmHg at 25°C |
| Index of Refraction | 1.641 |
