676484
VEGFR2 Kinase Inhibitor VI, Ki8751
Vascular Endothelial Growth Factor Receptor 2 Kinase Inhibitor VI, N-(2,4-Difluorophenyl)-N′-(4-(6,7-dimethoxy-4-quinolyloxy)-2-fluorophenyl)urea, VEGFR Tyrosine Kinase Inhibitor XXIV
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Merck KGaA
Frankfurter Str. 250
64293 Darmstadt
Germany
Phone: +49 6151 72-0
Fax: +49 6151 72 2000
19 June 2013
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| Product number | Qty/Pk |
|---|---|
| 676484-5MG | 5 mg |
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 µM, 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.
| Product information | |||
|---|---|---|---|
| Form | Off-white solid | ||
| Molar mass | 469.4 | ||
| Protect from Light | Yes | ||
| Packaged under inert gas | Yes | ||
| Purity | ≥97% by HPLC | ||
| Solubility | DMSO | ||
| Chemical formula | C24H18F3N3O4 | ||
| CAS number | 228559-41-9 | ||
| Store and ship information | |||
|---|---|---|---|
| Storage | +2°C to +8°C | ||
| Ship |
Ambient Temperature Only
Regulatory Review |
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| Safety information | |||
|---|---|---|---|
| S Phrase |
S: 22-24/25-36/37/39 Do not breathe dust. Avoid contact with skin and eyes. Wear suitable protective clothing, gloves and eye/face protection. |
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