tcsc2976 NVP-TNKS656

NVP-TNKS656 is a highly potent, selective, and orally active TNKS2 inhibitor with IC₅₀ of 6 nM, and is > 300 fold selectivity against PARP1 and PARP2.

IC50 & Target: IC50: 6 nM (TNKS2)^[1]

In Vivo: NVP-TNKS656 (30 or 100 mg/kg, p.o.) exhibits good exposure and moderate oral bioavailability of 32% and 53%, respectively. Some slight overproportional increase in oral exposure is observed between 30 and 100 mg/kg with the dose normalized AUC for the 100 mg/kg dose being 2-fold higher than for the 30 mg/kg dose. Mice treated with NVP-TNKS656 (350 mg/kg, p.o.) show good plasma and tumor exposures corresponding to AUC_0-24h of 515 and 325 μM·h, respectively^[1].