Home Tools
Log in
Cart

KI8751

Catalog No. T2446   CAS 228559-41-9

KI8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
KI8751 Chemical Structure
KI8751, CAS 228559-41-9
Pack Size Availability Price/USD Quantity
2 mg In stock $ 31.00
5 mg In stock $ 48.00
10 mg In stock $ 78.00
25 mg In stock $ 158.00
50 mg In stock $ 310.00
100 mg In stock $ 543.00
200 mg In stock $ 706.00
500 mg In stock $ 1,080.00
1 mL * 10 mM (in DMSO) In stock $ 51.00
Bulk Inquiry
Get quote
Select Batch  
Purity: 99.9%
Purity: 99.73%
Contact us for more batch information
Biological Description
Chemical Properties
Storage & Solubility Information
Description KI8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM.
Targets&IC50 VEGFR2:0.9 nM
Kinase Assay Cellular Kinase Assays: NIH3T3 cells prepared by transfection of human KDR. The cells are cultured in a collagen type I coated 96-well plate in an amount of 1.5 × 104 per well. The medium is then replaced by a DMEM medium containing 0.1% FCS. Ki8751 diluted in DMSO is added to each well and cultured. rhVEGF is added to a final concentration of 100 ng/mL, and the stimulation of cells is carried out at 37 °C. The cells are washed with PBS (pH 7.4), 50 μL of a solubilization buffer (20 mM HEPES (pH 7.4), 150 mM NaCl, 0.2% Triton X-100, 10% glycerol, 5 mM Na3VO4, 5 mM disodium ethylenediamine tetraacetate, and 2 mM Na4P2O7) is then added and a cell extract is prepared. Separately, PBS (50 μL, pH 7.4) containing 5 μg/mL of antiphosphotyrosine antibody (PY20) is added to a microplate for ELISA. After washing of the plate, 300 μL of a blocking solution is added. The cell extract is transferred to the plate. An anti-VEGFR2 antibody and a peroxidase-labeled anti-rabbit Ig antibody are added. Next, a chromophoric substrate for peroxidase is added, and the absorbance at 450 nm is measured with microplate reader. The VEGFR2 phosphorylation activity for each well is determined by presuming the absorbance with the addition of VEGF and without the addition of the test sample to be 100% VEGFR2 phosphorylation activity and VEGF to be 0% VEGFR2 phosphorylation activity. The concentration of the inhibition (%) of VEGFR2 Phosphorylation is determined for each case, and IC50 value is calculated.
Cell Research To evaluate the inhibition of VEGF-Stimulated HUVEC proliferation by Ki8751, HUVECs are plated at a density of 4000 cells/200 μL/well in a type I collagen pre-coated 96-well plates. After 24 hours, the cells are incubated for 1 hour with Ki8751 and then stimulated with 20 ng/mL rhVEGF. The cultures are incubated at 37 °C for 72 hours, then pulsed with 1 μCi/well [3H]thymidine and re-incubated for 14 hours. Cells are assayed for the incorporation of tritium using a beta counter. (Only for Reference)
Molecular Weight 469.41
Formula C24H18F3N3O4
CAS No. 228559-41-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 46.9 mg/mL (100 mM)

TargetMolReferences and Literature

1. Kubo K, et al. J Med Chem, 2005, 48(5), 1359-1366. 2. Tamura D, et al. Cancer Sci, 2010, 101(6), 1403-1408. 3. Hasan MR, et al. Int J Cancer, 2011, 129(9), 2115–2123.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Lung Cancer Compound Library Anti-Breast Cancer Compound Library Anti-Fibrosis Compound Library JAK-STAT Compound Library Tyrosine Kinase Inhibitor Library Bioactive Compounds Library Max Immunology/Inflammation Compound Library Anti-Liver Cancer Compound Library Angiogenesis related Compound Library Cytokine Inhibitor Library

Related Products

Related compounds with same targets
BMS-599626 JAK 3 inhibitor IV Naquotinib mesylate Chamigrenal Astragaloside VI BMS-690514 4-Hydroxycinnamamide EGFR mutant-IN-1

TargetMolDose Conversion

You can also refer to dose conversion for different animals. More

TargetMol In vivo Formulation Calculator (Clear solution)

Step One: Enter information below
Dosage
mg/kg
Average weight of animals
g
Dosing volume per animal
ul
Number of animals
Step Two: Enter the in vivo formulation
% DMSO
%
% Tween 80
% ddH2O
Calculate Reset

TargetMolCalculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculation
Molecular Weight Calculator
=
X
X

Molarity Calculator allows you to calculate the

  • Mass of a compound required to prepare a solution of known volume and concentration
  • Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Concentration of a solution resulting from a known mass of compound in a specific volume
See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

X
=
X

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

=
/

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

KI8751 228559-41-9 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR FGFR VEGFR PDGFR c-Kit inhibit KI-8751 KI 8751 Ki 8751 Inhibitor Vascular endothelial growth factor receptor inhibitor

 

TargetMol