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JW 74
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
JW 74图片
CAS NO:863405-60-1
规格:98%
分子量:456.5
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍
inhibitor of the catalytic PARP domain of TNKS1/2
CAS:863405-60-1
分子式:C24H20N6O2S
分子量:456.5
纯度:98%
存储:Store at -20°C

Background:

IC50: 790 nM for canonical Wnt signaling


JW 74 is an inhibitor of the catalytic PARP domain of TNKS1/2.


Wnt/β-catenin, a major regulator of stem cell self-renewal and differentiation, is aberrantly activated in a several cancers, including osteosarcoma. Thus, attenuation of Wnt/β-catenin activity by tankyrase inhibitors is an appealing strategy in osteosarcoma treatment.


In vitro: Previous study found that JW74 at the molecular level induced stabilization of AXIN2, a key component of the β-catenin destruction complex, leading to reduced levels of nuclear β-catenin. In addition, JW74 could induce reduced cell growth in all tested cell lines, partially due to a delay in cell cycle progression and partially because of an induction of caspase-3-mediated apoptosis. Moreover, JW74 was able to induce the differentiation in U2OS cells and also enhance differentiation of OS cell lines that did not harbor a differentiation block [1].


In vivo: Previous animal study found that the dose of 150 mg/kg of JW74 in ApcMin model could reduce the small intestinal adenoma by 48% and was comparable with celecoxib or rofecoxib. Furthermore, it was noteworthy that JW74 became rapidly cleared from the blood stream due to its poor in vivo stability [2].


Clinical trial: Up to now, JW 74 is still in the preclinical development stage.


参考文献:
1.  E. W. Stratford, J. Daffinrud, E. Munthe, et al. The tankyrase-specific inhibitor JW74 affects cell cycle progression and induces apoptosis and differentiation in osteosarcoma cell lines. Cancer Med. 3(1), 36-46 (2014).
2.  Waaler J et al. Novel synthetic antagonists of canonical Wnt signaling inhibit colorectal cancer cell growth. Cancer Res. 2011 Jan 1;71(1):197-205.