RK-582 is a tankyrase inhibitor, antitumor agent, and orally bioavailable growth inhibitor, with an IC 50 of 36.1 nM against human tankyrase-1 and an IC 50 of 39.2 nM against human tankyrase-2 . In APC-mutated colorectal cancer cells, the sensitivity to RK-582 correlates with the level of active β-catenin , while drug resistance associates with PIK3CA mutation. RK-582 can be used for the research of colorectal cancer .
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