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RKI-1447

Cat. No. M2148

RKI-1447 Structure
Size Price Availability Quantity
10mg USD 120 In stock
50mg USD 450 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.

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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 326.37
Formula C16H14N4O2S
CAS Number 1342278-01-6
Purity 98.80%
Solubility DMSO
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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