JK-P3

Modify Date: 2024-02-28 11:08:56

JK-P3 Structure
JK-P3 structure
Common Name JK-P3
CAS Number 942655-44-9 Molecular Weight 323.35
Density 1.3±0.1 g/cm3 Boiling Point 499.6±45.0 °C at 760 mmHg
Molecular Formula C18H17N3O3 Melting Point N/A
MSDS Chinese USA Flash Point 255.9±28.7 °C
Symbol GHS07
GHS07
Signal Word Warning

 Use of JK-P3


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].

 Names

Name JK-P3
Synonym More Synonyms

 JK-P3 Biological Activity

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

[1]. Kankanala J, et al. A combinatorial in silico and cellular approach to identify a new class of compounds that target VEGFR2 receptor tyrosine kinase activity and angiogenesis. Br J Pharmacol. 2012;166(2):737-748.

 Chemical & Physical Properties

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

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302
RIDADR NONH for all modes of transport

 Synonyms

Benzamide, 3,4-dimethoxy-N-(3-phenyl-1H-pyrazol-5-yl)-
3,4-Dimethoxy-N-(3-phenyl-1H-pyrazol-5-yl)benzamide