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KRN 633 is a cell-permeable, reversible, ATP-competitive VEGFR kinase inhibitor with IC50 of 170 nM, 160 nM, and 125 nM for VEGFR-1, VEGFR-2, VEGFR-3, respectively. It inhibits PDGFR-α and c-Kit at higher concentrations only (IC50 = 0.97 µM and 4.33 µM, respectively) and inactive towards 17 other kinases (IC50 ≥ 10 µM). Shown to suppress VEGF-dependent, but not FGF-dependent, cellular signaling and cell proliferation. Although not cytotoxic to cancer cells, KRN633 exhibits excellent in vivo antitumor activity due to its inhibitory effects on vessel formation and vascular permeability.
| Cell Experiment | |
|---|---|
| Cell lines | A549, Ls174T, DU145, HT29, LNCap and PC-3 cell lines |
| Preparation method | Plating cancer cells in media containig 10% FBS and antibiotics, at densities known to permit exponential growth over the assay period. Culturing the cells for 24 hours before adding KRN633 (0.01 to 10 μM) or just the vehicle (0.1% DMSO in medium) and then growing for a further 96 hours. Using WST-1 reagent to measure cell viability . |
| Concentrations | Dissolved in DMSO, final concentrations 0.01 to 10 μM |
| Incubation time | 96 hours |
| Animal Experiment | |
|---|---|
| Animal models | A549, Ls174T, HT29, DU145, LNCap, PC-3 cells and LC-6-JCK are established in athymic mice (BALB/cA, Jcl-nu) and athymic rats (F344/N, Jcl-rnu), respectively. |
| Formulation | Suspended in vehicle (0.5% methylcellulose solution) |
| Dosages | 20-100 mg/kg |
| Administration | Gavage once daily |
| Molecular Weight | 416.86 |
| Formula | C20H21ClN4O4 |
| CAS Number | 286370-15-8 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[3] Akane Morita, et al. Establishment of an abnormal vascular patterning model in the mouse retina
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