化合物NVP-TNKS656 T3261

Product Introduction
Bioactivity


英文名: NVP-TNKS656

描述: NVP-TNKS656 (TNKS656) 是一种可口服的选择性TNKS2抑制剂，IC50值为 6 nM。

体外活性: 体外研究显示，NVP-TNKS656在不同物种中的微粒体ER值较低至中等，并且具有较高的溶解性。[1] 在对PI3K或AKT抑制剂具有抗性的细胞中，NVP-TNKS656阻断Wnt/β-Catenin途径并促进细胞凋亡。[2]

体内活性: In mice, NVP-TNKS656 displays low clearance and volume of distribution, and exhibits good exposure and moderate oral bioavailability. In MMTV-Wnt1 tumor bearing athymic nude mice, NVP-TNKS656 (350 mg/kg, p.o.) stabilizes Axin1 protein and reduces the Wnt/beta-catenin target gene Axin2 mRNA level by 70-80%. [1] In colorectal cancer PDX models, NVP-TNKS656 reduces nuclear β-catenin, reverts such resistance, and represses tumor growth. [2]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 93 mg/mL (188 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 10 mg/mL(20.21 mM)


关键字: NVPTNKS656 | Inhibitor | PARP | inhibit | Apoptosis | poly ADP ribose polymerase | NVP TNKS656 | NVP-TNKS-656 | NVP-TNKS 656 | TNKS-656 | TNKS 656 | NVP-TNKS656

相关产品: JNJ-7706621 | Declopramide | Citicoline sodium | 2,5-dimethyl Celecoxib | kauran-16,17-diol | ROC-325 | (-)-Anonaine | SRT 2183 | NQDI-1 | Pictilisib

相关库: Anti-Prostate Cancer Compound Library | Anti-Breast Cancer Compound Library | Anti-Cancer Metabolism Compound Library | Neuronal Differentiation Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Highly Selective Inhibitor Library | DNA Damage & Repair Compound Library | Metabolism Compound Library | NO PAINS Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途