1. Protein Tyrosine Kinase/RTK
  2. VEGFR FGFR
  3. 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.

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

JK-P3 Chemical Structure

JK-P3 Chemical Structure

CAS No. : 942655-44-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 77 In-stock
Solution
10 mM * 1 mL in DMSO USD 77 In-stock
Solid
5 mg USD 70 In-stock
10 mg USD 125 In-stock
25 mg USD 270 In-stock
50 mg USD 480 In-stock
100 mg USD 750 In-stock
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (154.63 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0926 mL 15.4631 mL 30.9262 mL
5 mM 0.6185 mL 3.0926 mL 6.1852 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.73 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.73 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0926 mL 15.4631 mL 30.9262 mL 77.3156 mL
5 mM 0.6185 mL 3.0926 mL 6.1852 mL 15.4631 mL
10 mM 0.3093 mL 1.5463 mL 3.0926 mL 7.7316 mL
15 mM 0.2062 mL 1.0309 mL 2.0617 mL 5.1544 mL
20 mM 0.1546 mL 0.7732 mL 1.5463 mL 3.8658 mL
25 mM 0.1237 mL 0.6185 mL 1.2370 mL 3.0926 mL
30 mM 0.1031 mL 0.5154 mL 1.0309 mL 2.5772 mL
40 mM 0.0773 mL 0.3866 mL 0.7732 mL 1.9329 mL
50 mM 0.0619 mL 0.3093 mL 0.6185 mL 1.5463 mL
60 mM 0.0515 mL 0.2577 mL 0.5154 mL 1.2886 mL
80 mM 0.0387 mL 0.1933 mL 0.3866 mL 0.9664 mL
100 mM 0.0309 mL 0.1546 mL 0.3093 mL 0.7732 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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JK-P3
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HY-108933
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