1. Protein Tyrosine Kinase/RTK
  2. VEGFR
    FGFR
  3. JK-P3

JK-P3 

Cat. No.: HY-108933
Handling Instructions

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.

For research use only. We do not sell to patients.

JK-P3 Chemical Structure

JK-P3 Chemical Structure

CAS No. : 942655-44-9

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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].

IC50 & Target[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

323.35

Formula

C18H17N3O3

CAS No.
SMILES

O=C(NC1=NNC(C2=CC=CC=C2)=C1)C3=CC=C(OC)C(OC)=C3

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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JK-P3
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