RK-287107

RK-287107 is an inhibitor of the tankyrases TNKS1 and TNKS2 (IC₅₀s = 0.014 and 0.010 µM, respectively).¹ It is selective for TNKS1 and TNKS2 over poly(ADP-ribose) polymerase 1 (PARP1), PARP2, and PARP10 (IC₅₀s = >20, 2.7, and 19.8 µM, respectively). RK-287107 inhibits Wnt-dependent signaling with an IC₅₀ value of 0.077 µM in a reporter assay. It increases accumulation of Axin2, indicating inhibition of TNKS-mediated auto-PARsylation, in COLO 320DM colorectal cancer cells when used at a concentration of 0.1 µM. RK-287107 also inhibits cell growth in the same model (GI₅₀ = 0.45 µM). It reduces tumor growth in a COLO 320DM mouse xenograft model when administered at a dose of 150 mg/kg twice per day.

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1. Shirai, F., Tsumura, T., Yashiroda, Y., et al. Discovery of novel spiroindoline derivatives as selective tankyrase inhibitors. J. Med. Chem. 62(7), 3407-3427 (2019).