RKI 1447 is a potent and selective ROCK inhibitor. It displays anti-invasive and antitumor activities in breast cancer cells. RKI-1447 can inhibit the proliferation, migration and invasion abilities of ovarian cancer cells. RKI 1447 exhibits cytotoxic and cytostatic effects on VHL-deficient clear cell renal cell carcinoma (CC-RCC), making them candidate novel therapeutics for CC-RCC. RKI-1447 significantly inhibited mammary tumor growth in animal models.