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RKI-1447

Cat. No. M2148
RKI-1447 Structure
Size Price Availability Quantity
5mg USD 79.2  USD88 In stock
10mg USD 108  USD120 In stock
50mg USD 414  USD460 In stock
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Quality Control
Biological Activity

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.

Customer Product Validations & Biological Datas
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 326.37
Formula C16H14N4O2S
CAS Number 1342278-01-6
Purity 98.80%
Solubility DMSO 55 mg/mL
Storage at -20°C
References

RKI-1447 is a potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and antitumor activities in breast cancer.
Patel RA, et al. Cancer Res. 2012 Oct 1;72(19):5025-34. PMID: 22846914.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: RKI-1447 supplier, ROCK, inhibitors

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