NVP-TNKS656

製品コードS7238 バッチS723802

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₇H₃₄N₄O₅

分子量

494.58

CAS No.

1419949-20-4

Solubility (25°C)*

体外

DMSO

100 mg/mL (202.19 mM)

Ethanol (warmed with 50ºC water bath)

10 mg/mL (20.21 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	NVP-TNKS656 is a highly potent, selective, and orally active tankyrase inhibitor with IC50 of 6 nM for TNKS2, > 300-fold selectivity against PARP1 and PARP2.
in vitro	In vitro, NVP-TNKS656 shows low to moderate microsomal ER values across species and high solubility. ^[1] In PI3K or AKT inhibitor-resistant cells, this compound blocks Wnt/β-Catenin pathway and promotes apoptosis. ^[2]
in vivo	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, this compound (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, this chemical reduces nuclear β-catenin, reverts such resistance, and represses tumor growth. ^[2]

製品説明

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

in vitro

In vitro, NVP-TNKS656 shows low to moderate microsomal ER values across species and high solubility. ^[1]

In PI3K or AKT inhibitor-resistant cells, this compound blocks Wnt/β-Catenin pathway and promotes apoptosis. ^[2]

in vivo

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, this compound (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, this chemical reduces nuclear β-catenin, reverts such resistance, and represses tumor growth. ^[2]

プロトコル(参考用のみ)

キナーゼアッセイ	Tankyrase AutoPARsylation Assay
キナーゼアッセイ	PARP catalytic activity is monitored using the quantitative liquid chromatography/mass spectrometry (LC-MS) detection of nicotinamide. The autoPARsylation reactions are performed at room temperature in 384-well Greiner flat-bottom plates. The final reaction mixture contains 2.5% DMSO and inhibitors with concentrations ranging from 0.0001 to 18.75 μM. GST-TNKS2P, GST-TNKS1P, PARP1, and PARP2 enzymes are used at final concentrations or 5, 5, 5, and 2 nM, respectively. The nicotinamide concentration in the resulting supernatants is measured by LC-MS. The % inhibition is calculated as follows: (control – sample)/(control – background) × 100. “Control” is the average value of eight wells without compound, and “background” is the average of eight wells mixed with 5× quenching solution measured prior to initiation of the reaction.
細胞アッセイ	細胞株	Cell-free assays
	濃度	6 nM
	反応時間
	実験の流れ
動物実験	動物モデル	Athymic female nude mice bearing MMTV-Wnt1 tumors
	投薬量	350 mg/kg
	投与方法	p.o.

参考

https://pubmed.ncbi.nlm.nih.gov/23844574/
https://pubmed.ncbi.nlm.nih.gov/26224873/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

WNK1 mediates M-CSF-induced macropinocytosis to enforce macrophage lineage fidelity [ Nat Commun, 2025, 16(1):4945]	PubMed: 40436823
Enhancer remodeling by OTX2 directs specification and patterning of mammalian definitive endoderm [ Dev Cell, 2025, S1534-5807(25)00496-4]	PubMed: 40834858
TNF-NF-κB-p53 axis restricts in vivo survival of hPSC-derived dopamine neurons [ Cell, 2024, 187(14):3671-3689.e23]	PubMed: 38866017
Systematic mapping and modeling of 3D enhancer-promoter interactions in early mouse embryonic lineages reveal regulatory principles that determine the levels and cell-type specificity of gene expression [ bioRxiv, 2023, 2023.07.19.549714]	PubMed: 37577543
Systematic mapping and modeling of 3D enhancer-promoter interactions in early mouse embryonic lineages reveal regulatory principles that determine the levels and cell-type specificity of gene expression [ bioRxiv, 2023, 2023.07.19.549714]	PubMed: 37577543
Identification of novel target for osteosarcoma by network analysis [ Med Sci Monit, 2018, 24: 5914–5924]	PubMed: 30144309
Identification of Novel Target for Osteosarcoma by Network Analysis [Zhi LQ, et al. Med Sci Monit, 2018, 24:5914-5924]	PubMed: 30144309

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。