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RKI-1447 is a potent and selective ROCK inhibitor with significant anti-invasive and antitumor activities. RKI-1447 binds the ATP binding site through interactions with the hinge region and the DFG motif. RKI-1447 inhibited migration, invasion and anchorage-independent tumor growth of breast cancer cells. RKI-1447 was also highly selective at inhibiting ROCK-mediated cytoskeleton re-organization (actin stress fiber formation) following LPA stimulation, but does not affect PAK-meditated lamellipodia and filopodia formation following PDGF and Bradykinin stimulation, respectively. RKI-1447 suppressed phosphorylation of the ROCK substrates MLC-2 and MYPT-1 in human cancer cells, but had no effect on the phosphorylation levels of the AKT, MEK and S6 kinase at concentrations as high as 10 μmol/L. Finally, RKI-1447 was highly effective at inhibiting the outgrowth of mammary tumors in a transgenic mouse model.
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Source | Neoplasia (2018). Figure 7. RKI-1447 |
| Method | 3D spheroid invasion assays | |
| Cell Lines | MSC-4H-FC cells | |
| Concentrations | 10 μM | |
| Incubation Time | 24 h | |
| Results | Importantly, concentrations of RKI-1447 as low as 0.5 μM were able to completely abolish the invasion of MSC-4H-FC 3D spheroids and to significantly reduce cell extravasation out of the CAM vasculature without having any relevant effect on cell proliferation. |
| Molecular Weight | 326.37 |
| Formula | C16H14N4O2S |
| CAS Number | 1342278-01-6 |
| Solubility (25°C) | DMSO 55 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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