Ki 8751

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Cat.No. 2542 - Ki 8751 | C24H18F3N3O4 | CAS No. 228559-41-9
Description: Potent, selective VEGFR-2 inhibitor
Chemical Name: N-(2,4-Difluorophenyl)-N'-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]-2-fluorophenyl]urea
Purity: ≥97% (HPLC)
Datasheet
Citations (1)
Literature
Pathways

Biological Activity

Potent, selective inhibitor of VEGFR-2 tyrosine kinase (IC50 = 0.9 nM). Displays some inhibitory activity towards c-Kit, PDGFRα and FGFR-2 (IC50 values range from 40 to 170 nM) but is highly selective over other receptor tyrosine kinases (IC50 > 10000 nM for FGFR-2, EGFR and HGFR). Inhibits VEGF-stimulated proliferation of human umbilical vein endothelial cells (HUVEC) and inhibits tumor growth in vivo; antiangiogenic.

Compound Libraries

Ki 8751 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 469.41
Formula C24H18F3N3O4
Storage Store at +4°C
Purity ≥97% (HPLC)
CAS Number 228559-41-9
PubChem ID 11317348
InChI Key LFKQSJNCVRGFCC-UHFFFAOYSA-N
Smiles COC1=C(OC)C=C2C(OC3=CC=C(NC(=O)NC4=CC=C(F)C=C4F)C(F)=C3)=CC=NC2=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 46.94 100

Preparing Stock Solutions

The following data is based on the product molecular weight 469.41. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.13 mL 10.65 mL 21.3 mL
5 mM 0.43 mL 2.13 mL 4.26 mL
10 mM 0.21 mL 1.07 mL 2.13 mL
50 mM 0.04 mL 0.21 mL 0.43 mL

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Reconstitution Calculator

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Kubo et al (2005) Novel potent orally active selective VEGFR-2 tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumour activities of N-phenyl-N'-{4-(4-quinolyloxy)phenyl}ureas. J.Med.Chem. 48 1359 PMID: 15743179


If you know of a relevant reference for Ki 8751, please let us know.

View Related Products by Product Action

View all VEGFR Inhibitors

Keywords: Potent selective VEGFR-2 inhibitors inhibits Vascular Endothelial Growth Factors Receptors KDR Flt Receptor Tyrosine Kinases RTKs Ki8751 VEGFR

1 Citation for Ki 8751

Citations are publications that use Tocris products. Selected citations for Ki 8751 include:

Kawakami et al (2011) Investigation of a novel molecular descriptor for the lead optimization of 4-aminoquinazolines as vascular endothelial growth factor receptor-2 inhibitors: application for quantitative structure-activity relationship analysis in lead optimization. J Neurosci 21 1371 PMID: 21306896


Do you know of a great paper that uses Ki 8751 from Tocris? If so please let us know.

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Reviews

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Angiogenesis in Cancer

Angiogenesis in Cancer Poster

Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.

Pathways for Ki 8751

VEGF

VEGF Signaling Pathway

VEGF signaling pathway is involved in embryonic vascular development (vasculogenesis) and in the formation of new blood vessel (angiogenesis). It also induces cell migration, proliferation and survival.

Protocols

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