NVP-TNKS656 (Synonyms: TNKS656) |
| Catalog No.GC17555 |
NVP-TNKS656은 IC50이 6nM인 매우 강력하고 선택적이며 경구 활성인 TNKS2 억제제이며 PARP1 및 PARP2에 대해 300배 이상의 선택성을 나타냅니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1419949-20-4
Sample solution is provided at 25 µL, 10mM.
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NVP-TNKS656 is an orally active antagonist of Wnt pathway activity. The Wnt pathway has been involved in controlling numerous developmental processes. Dysfunction of this pathway may result in carcinogenesis [1].
In vitro: The IC50 value of NVP-TNKS656 against PARP1, TNKS2, PARP2, and STF was > 19, 0.006, 32, and 0.0035 µM, respectively [1].
In vivo: The clearance and volume of distribution of NVP-TNKS656 were 10 mL/min/kg and 0.6 L/kg after intravenous administration in mice. The exposure and oral bioavailability was 32% and 53%, respectively. In the mouse mammary tumor virus (MMTV)-Wnt1 transgenic model, oral administration of NVP-TNKS656 (350 mg/kg) activated the Wnt signaling over a 24-h time course. NVP-TNKS656 treatment reduced the Wnt/beta-catenintarget gene Axin2 mRNA level by 70-80% [1].
Reference:
Shultz M D, Cheung A K, Kirby C A, et al. Identification of NVP-TNKS656: the use of structure-efficiency relationships to generate a highly potent, selective, and orally active tankyrase inhibitor[J]. Journal of medicinal chemistry, 2013, 56(16): 6495-6511.
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