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
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	Research Areas >> Cancer Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FGFR Signaling Pathways >> Protein Tyrosine Kinase/RTK >> VEGFR
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.

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

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

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