KI8751

SKU: orb1305473

Description

KI8751 is a highly potent and selective small molecule inhibitor targeting VEGFR2, demonstrating an IC50 value of 0.9 nM. It is widely used in preclinical research to study angiogenesis, tumor growth, and metastasis in both cellular assays and animal models.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 228559-41-9
• MW: 469.41
• Purity: 99.90% (May vary between batches)
• Formula: C₂₄H₁₈F₃N₃O₄
• SMILES: COc1cc2nccc(Oc3ccc(NC(=O)Nc4ccc(F)cc4F)c(F)c3)c2cc1OC
• Target: c-Kit,VEGFR,FGFR,EGFR,PDGFR
• Solubility: DMSO:14 mg/mL (29.82 mM);10% DMSO+90% Corn Oil:1 mg/mL (2.13 mM)

Bioactivity

• Target IC50:
  VEGFR2:0.9 nM
• In Vivo:
  In human umbilical vein endothelial cells (HUVECs), Ki8751 (1 nM-100 nM) effectively reduced VEGF-stimulated cell proliferation and vascular permeability. In metastatic colorectal cancer (CRC) cells MIP, RKO, SW620 and SW480, Ki8751 (10 nM) increased cellular senescence, but not in HCT116.Ki8751 potently and selectively inhibited VEGFR-2 with an IC50 of 0.9 nM.Ki8751 also inhibited PDGFRα, c-Kit and FGFR-2 with higher IC50. Ki8751 also inhibits PDGFRα, c-Kit and FGFR-2, with higher IC50 values of 40 nM-170 nM.
• In Vitro:
  In human umbilical vein endothelial cells (HUVECs), Ki8751 (1 nM-100 nM) effectively reduced VEGF-stimulated cell proliferation and vascular permeability. In metastatic colorectal cancer (CRC) cells MIP, RKO, SW620 and SW480, Ki8751 (10 nM) increased cellular senescence, but not in HCT116.Ki8751 potently and selectively inhibited VEGFR-2 with an IC50 of 0.9 nM.Ki8751 also inhibited PDGFRα, c-Kit and FGFR-2 with higher IC50. Ki8751 also inhibits PDGFRα, c-Kit and FGFR-2, with higher IC50 values of 40 nM-170 nM.
• 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)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

c-Kit, cKit, inhibit, Inhibitor, KI8751, KI-8751, KI 8751, Ki 8751, EGFR, FGFR2, PDGFRα, Vascular endothelial growth factor receptor, VEGFR2, VEGFR

Compound Identifiers

PubChem CID

11317348