1. Protein Tyrosine Kinase/RTK
  2. VEGFR
  3. Ki8751

Ki8751 

Cat. No.: HY-12038 Purity: 98.97%
Handling Instructions

Ki8751 is a potent VEGFR2 inhibitor with an IC50 of 0.9 nM.

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

Ki8751 Chemical Structure

Ki8751 Chemical Structure

CAS No. : 228559-41-9

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 101 In-stock
Estimated Time of Arrival: December 31
10 mg USD 92 In-stock
Estimated Time of Arrival: December 31
50 mg USD 378 In-stock
Estimated Time of Arrival: December 31
100 mg USD 666 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Ki8751 purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Sep 24;9(10):982.

    Western blot is performed to detect the expression of VEGFR2, p-VEGFR2, Akt, p-Akt, mTOR, p-mTOR, E-cadherin, Vimentin, and N-cadherin after adding Ki8751 to HCT116, and HCT8 cells.

    View All VEGFR Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Ki8751 is a potent VEGFR2 inhibitor with an IC50 of 0.9 nM.

    IC50 & Target[1]

    VEGFR2

    0.9 nM (IC50)

    In Vitro

    Ki8751 inhibits VEGFR-2 phosphorylation at an IC50 value of 0.90 nM, and also inhibits the PDGFR family members such as PDGFRR and c-Kit at 67 nM and 40 nM, respectively. However, Ki8751 does not have any inhibitory activity against other kinases such as EGFR, HGFR, InsulinR and others even at 10000 nM. Ki8751 suppresses the growth of the VEGF-stimulated human umbilical vein endothelial cell (HUVEC) on a nanomolar level[1].

    In Vivo

    Ki8751 shows significant antitumor activity against five human tumor xenografts such as GL07 (glioma), St-4 (stomach carcinoma), LC6 (lung carcinoma), DLD-1 (colon carcinoma) and A375 (melanoma) in nude mice and also shows complete tumor growth inhibition with the LC-6 xenograft in nude rats following oral administration once a day for 14 days at 5 mg/kg without any body weight loss[1].

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 92 mg/mL (195.99 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1303 mL 10.6517 mL 21.3033 mL
    5 mM 0.4261 mL 2.1303 mL 4.2607 mL
    10 mM 0.2130 mL 1.0652 mL 2.1303 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

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

      Solubility: 2.5 mg/mL (5.33 mM); Suspended solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.33 mM); Clear solution

    • 3.

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

      Solubility: 2.5 mg/mL (5.33 mM); Suspended solution; Need ultrasonic

    *All of the co-solvents are provided by MCE.
    References
    Kinase Assay
    [1]

    VEGFR-2 kinase assay is described below; GST-fusion proteins of KDR (Flk-1: cytoplasmic domain) are produced in the baculo-virus expression system. GST-KDR is premixed with a serial dilution of Ki8751 in the kinase buffer. The kinase reaction is initiated by the addition of 2 µM ATP in a solution of MnCl2. After 20 min incubation at room temperature, the reaction is stopped with an addition of EDTA. Phosphorylation levels of GST-KDR are detected by immunoblotting with anti-phosphotyrosine monoclonal antibodies (PY20) and detected by ECL fluorography[1].

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

    Cell Assay
    [1]

    HUVECs are placed at a density of 4000 cells/200 µL/well on collagene type I precoated 96-well plates in M199 medium with 5% fetal bovine serum (FBS). After 24 h, the cells are incubated for 1 h in the presence or absence of Ki8751; then the cells are stimulated by rhVEGF (20 ng/mL). The cultures are incubated at 37 °C for 72 h, then pulsed with 1 µCi/well [3H]thymidine and reincubated for 14 h. Cells are assayed for the incorporation of tritium using a beta counter[1].

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

    Animal Administration
    [1]

    Mice: The effects of Ki8751 on tumor growth is tested against various tumors, human stomach carcinoma (St-4), human lung carcinoma (LC-6), human colon carcinoma (DLD-1) and human melanoma (A375), using human tumor xenografts in nude mice. Ki8751 is administered orally to mice in the experimental groups once a day for 9 consecutive days at 5 mg/kg, and the vehicle is administered to control animals. Tumor volumes are monitored twice weekly[1].

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

    References
    Molecular Weight

    469.41

    Formula

    C₂₄H₁₈F₃N₃O₄

    CAS No.

    228559-41-9

    SMILES

    COC1=CC2=C(C=CN=C2C=C1OC)OC3=CC=C(C(F)=C3)NC(NC4=CC=C(C=C4F)F)=O

    Shipping

    Room temperature in continental US; may vary elsewhere

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    Inquiry Information

    Product Name:
    Ki8751
    Cat. No.:
    HY-12038
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    Ki8751

    Cat. No.: HY-12038