676484

VEGFR2 Kinase Inhibitor VI, Ki8751

The VEGFR2 Kinase Inhibitor VI, Ki8751, also referenced under CAS 228559-41-9, controls the biological activity of VEGFR2 Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): VEGFR2 Kinase Inhibitor VI, Ki8751, N-(2,4-Difluorophenyl)-Nʹ-(4-(6,7-dimethoxy-4-quinolyloxy)-2-fluorophenyl)urea, Vascular Endothelial Growth Factor Receptor 2 Kinase Inhibitor VI, VEGFR Tyrosine Kinase Inhibitor XXIV
• Empirical Formula (Hill Notation): C₂₄H₁₈F₃N₃O₄
• CAS Number: 228559-41-9
• Molecular Weight: 469.41
• MDL number: MFCD09971092
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥97% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Properties

• Quality Segment: 100
• assay: ≥97% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: off-white
• solubility: DMSO: 50 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: Fc1c(ccc(c1)F)NC(=O)Nc2c(cc(cc2)Oc3c4c(ncc3)cc(c(c4)OC)OC)F
• InChI: 1S/C24H18F3N3O4/c1-32-22-11-15-20(12-23(22)33-2)28-8-7-21(15)34-14-4-6-19(17(27)10-14)30-24(31)29-18-5-3-13(25)9-16(18)26/h3-12H,1-2H3,(H2,29,30,31)
• InChI key: LFKQSJNCVRGFCC-UHFFFAOYSA-N

Description

General description

A cell-permeable quinolyloxyphenyl-urea compound that acts as a VEGFR-2-selective inhibitior in both cell-based (IC₅₀ = 0.9 nM in VEGF-induced receptor phosphorylation) and cell-free (IC₅₀ = 4.0 nM in kinase reactions) assays. It inhibits c-Kit, PDGFRα, and FGFR-2 only at much higher concentrations (IC₅₀ = 40, 67, and 170 nM, respectively, in cell-based assays), while exhibiting no effect against eight other commonly studied receptor and non-receptor kinases even at concentrations as high as 10 µM. Effectively blocks VEGF-dependent, but not VEGF-independent, cell proliferation in vitro and tumor growth in mice and rats (5 to 20 mg/kg, daily p.o.) in vivo.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Kubo, K., et al. 2005. J. Med. Chem.48, 1359.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Regulatory Review (Z)

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk: WGK 1
• flash_point_f: Not applicable
• flash_point_c: Not applicable