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Chemical Structure| 228559-41-9 Chemical Structure| 228559-41-9

Structure of Ki8751
CAS No.: 228559-41-9

Chemical Structure| 228559-41-9

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Ki8751 is a selective VEGFR2 inhibitor with IC50 of 0.9 nM.

4.5 *For Research Use Only !

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Product Details of Ki8751

CAS No. :228559-41-9
Formula : C24H18F3N3O4
M.W : 469.41
SMILES Code : O=C(NC1=CC=C(OC2=CC=NC3=CC(OC)=C(OC)C=C23)C=C1F)NC4=CC=C(F)C=C4F
MDL No. :MFCD09971092
InChI Key :LFKQSJNCVRGFCC-UHFFFAOYSA-N
Pubchem ID :11317348

Safety of Ki8751

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Ki8751

RTK

Isoform Comparison

Biological Activity

Target
  • VEGFR2

    VEGFR2, IC50:0.9 nM

  • PDGFRα

    PDGFRα, IC50:67 nM

  • c-Kit

    c-Kit, IC50:40 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
HIMECs 4.7 μg/mL 30 minutes Ki8751 inhibited IL-17C CM-induced HIMEC migration. Cells. 2020 Jun 1;9(6):1363.
HeLa S3 cells 10 µM 2 days Ki8751 suppressed cell proliferation and caused nuclear shape changes, including binuclei and micronuclei. Int J Mol Sci. 2018 Dec 12;19(12):4014.
U87 cells 2.5 µM 24 hours Ki8751 treatment increased the expression of mitochondrial-related proteins in U87 cells, indicating that VEGFR2 inhibition suppresses glioblastoma cell proliferation by enhancing mitochondrial biogenesis. J Transl Med. 2024 May 3;22(1):419.
MCF-7 2.5 µM and 5 µM 24, 48, and 72 hours Ki8751 significantly reduced cancer cell proliferation and enhanced breast cancer cell apoptosis. Cancer Biol Med. 2021 Feb 15;18(1):139-154.
MDA-MB-231 2.5 µM and 5 µM 24, 48, and 72 hours Ki8751 significantly reduced cancer cell proliferation and enhanced breast cancer cell apoptosis. Cancer Biol Med. 2021 Feb 15;18(1):139-154.
HeLa S3 cells 1 µM 3 hours Ki8751 delayed M phase progression, causing misalignment of chromosomes and rotation of the mitotic spindle. Int J Mol Sci. 2018 Dec 12;19(12):4014.
U38 cells 2.5 µM 48 hours Ki8751 treatment increased the expression of mitochondrial-related proteins in U38 cells, indicating that VEGFR2 inhibition suppresses glioblastoma cell proliferation by enhancing mitochondrial biogenesis. J Transl Med. 2024 May 3;22(1):419.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rats Middle cerebral artery occlusion-induced cerebral ischemia-reperfusion injury model Tail vein injection 0.5 mg/kg Single dose 30 minutes prior to surgery Ki8751 reversed the angiogenesis and protective effects induced by TQHXD through inhibition of VEGFR2 activity, decreasing both p-FAK and p-Paxillin protein levels. Front Pharmacol. 2021 Jan 11;11:572624
Mice C57BL/6 mice Perfusion 1 nM Single administration Ki8751 significantly decreased outflow facility, with an average reduction of 34% (CI: -56, -2%; P=0.04, n=6). Invest Ophthalmol Vis Sci. 2017 Mar 1;58(3):1899-1908
Mice DLD-1 cell xenograft model Subcutaneous injection 10 μg/tumor Daily for 10 days Ki8751 suppressed IL-17C-induced tumor growth and angiogenesis. Cells. 2020 Jun 1;9(6):1363.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.13mL

0.43mL

0.21mL

10.65mL

2.13mL

1.07mL

21.30mL

4.26mL

2.13mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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