Successful, we will reply to you quickly.

OK

Please select the quantity.

OK

Your message is being sent, please wait.

Close

test

Close

Send mail failed, please send again!

Close

Products are for research use only. Not for human use. We do not sell to patients.

Signaling Pathway

Ki8751

HY-12038

(Ki 8751; Ki-8751)

Ki8751

Ki8751 Chemical Structure

Ki8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM, >40-fold selective for VEGFR2 than c-Kit, PDGFRα and FGFR-2, little activity to EGFR, HGFR and InsR.

Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO $85 In-stock
10 mg $77 In-stock
50 mg $315 In-stock
100 mg $555 In-stock
200 mg Get quote
500 mg Get quote
Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO €83 In-stock
10 mg €75 In-stock
50 mg €309 In-stock
100 mg €544 In-stock
200 mg Get quote
500 mg Get quote

* Please select Quantity before adding items.

Bulk Inquiry

Inquiry Information
Product name: Ki8751
Cat. No.: HY-12038

Ki8751 Data Sheet

  • View current batch:

    Purity: 99.68%

  • Pdf Version Network Version

    DataSheet

    Pdf Version Network Version

    MSDS

    Pdf Version

    COA

    Pdf Version

    NMR

    Pdf Version

    LCMS

Related Compound Libraries

Biological Activity of Ki8751

Ki8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM, >40-fold selective for VEGFR2 than c-Kit, PDGFRα and FGFR-2, little activity to EGFR, HGFR and InsR.
IC50 value: 0.9 nM [1]
Target: VEGFR2
in vitro: Ki8751 potently and selectively inhibits VEGFR2 with IC50 of 0.9 nM. Ki8751 also inhibits PDGFRα, c-Kit, and FGFR-2, with much higher IC50 values (40 nM–170 nM). Except for these several kinases, Ki8751 doesn't disturb other kinases, including HGFR, EGFR, and InsulinR, even at 10 μM [1]. In human umbilical vein endothelial cells (HUVECs), Ki8751 (1 nM–100 nM) effectively decreases VEGF-stimulated cell proliferation and vasculature permeability [2]. In metastatic colorectal cancer (CRC) cells MIP, RKO, SW620, and SW480, but not in HCT116, Ki8751 (10 nM) increases cellular senescence [3].
in vivo: In nude mice bearing human tumor xenografts of GL07, St-4, LC6, DLD-1, and A375 cells, Ki8751 (20 mg/kg) inhibits tumor growth. In nude rat xenograft models of LC-6 cells, Ki8751 (5 mg/kg) completely inhibits tumor growth without affecting body weight [1].

Protocol (Extracted from published papers and Only for reference)

More

Chemical Information

M.Wt 469.41 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C24H18F3N3O4
CAS No 228559-41-9
Solvent & Solubility

DMSO ≥92mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL

Preparing Stock Solutions

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

References on Ki8751

Inhibitor Kit

Related VEGFR Products

  • 2,4-Pyrimidinediamine with linker

    2,4-Pyrimidinediamine with linker is a patent compound in WO2013055780A1, Page 71; multikinase inhibitor and has a -NH2 terminal linker for further synthesis.

  • Altiratinib

    Altiratinib(DCC-2701) is a novel c-MET/TIE-2/VEGFR inhibitor; effectively reduce tumor burden in vivo and block c-MET pTyr(1349)-mediated signaling, cell growth and migration as compared with a HGF antagonist in vitro.

  • Apatinib

    Apatinib(YN-968D1) is an orally bioavailable, selective VEGFR2 inhibitor with IC50 of 1 nM.

  • Axitinib

    Axitinib(AG013736) blocked phosphorylation of VEGFR-2 and VEGFR-3 with average IC50s of 0.2 and 0.1 to 0.3 nM.

  • AZD2932

    AZD2932 is a new series of quinazoline ether inhibitor which potently inhibits VEGFR-2 and PDGFR with IC50s of 4 nM/8 nM/ 7 nM for PDGFR(beta)/VEGFR-2/Flt-3.

  • BMS-690514

    BMS-690514 is a potent and selective inhibitor of epidermal growth factor receptor (EGFR), HER2, and HER4, as well as the VEGF receptor kinases.

  • BMS-794833

    BMS-794833 is a potent ATP competitive inhibitor of Met/VEGFR2 with IC50 of 1.7/15 nM; also inhibits Ron, Axl and Flt3 with IC50 of <3 nM; a prodrug of BMS-817378.

  • E-3810

    E-3810 is a novel dual inhibitor targeting human vascular endothelial growth factor receptors (VEGFRs) and fibroblast growth factor receptors (FGFRs) with antiangiogenic activity.

  • E-7050

    E7050(Golvatinib) is a dual c-Met and VEGFR-2 inhibitor with IC50 of 14 nM and 16 nM.

  • EG00229

    EG00229 is the first small molecule inhibitors of the neuropilin-1 and VEGF-A interaction with an IC50 of inhibition of 8 uM(125I-VEGF binding to PAE/NRP1 cells).

MORE