RK-582 is a tankyrase inhibitor, antitumor agent, and orally bioavailable growth inhibitor. It has an IC50 of 36.1 nM against human tankyrase-1 and 39.2 nM against human tankyrase-2. In APC-mutated colorectal cancer cells, sensitivity to RK-582 correlates with the level of active β-catenin, while drug resistance is associated with PIK3CA mutation. RK-582 can be used for the research of colorectal cancer.
- Tankyrase inhibitor
- Antitumor agent
- Orally bioavailable growth inhibitor
- IC50 of 36.1 nM against human tankyrase-1
- IC50 of 39.2 nM against human tankyrase-2
- Correlates with active β-catenin levels in APC-mutated colorectal cancer cells
- Useful for colorectal cancer research