"目录号: HY-13990
Cell Cycle/DNA DamageEpigenetics-
NVP-TNKS656 是一种有效的，可口服的，选择性的TNKS2抑制剂，IC50值为 6 nM，是PARP1和PARP2的选择性的 300 多倍。
PARP
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生物活性
Description
NVP-TNKS656 is a highly potent, selective, and orally activeTNKS2inhibitor withIC50of 6 nM, and is > 300 fold selectivity againstPARP1andPARP2.
IC50& Target
IC50: 6 nM (TNKS2)
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 AUC0-24hof 515 and 325 μM·h, respectively[1].
References
[1].Shultz MD, et al. Identification of NVP-TNKS656: the use of structure-efficiency relationships to generate a highly potent, selective, and orally active tankyrase inhibitor. J Med Chem. 2013 Aug 22;56(16):6495-511.