NU1025

製品コードS7730 バッチS773002

印刷

化学情報

Synonyms

NSC 696807

Storage
(From the date of receipt)

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

化学式

C₉H₈N₂O₂

分子量

176.17

CAS No.

90417-38-2

Solubility (25°C)*

体外

DMSO

35 mg/mL (198.67 mM)

Ethanol (warmed with 50ºC water bath)

9 mg/mL (51.08 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.
Clear solution	40% PEG 400 1 saline この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	10.000mg/ml (56.76mM)	Taking the 1 mL working solution as an example, take 10 mg of the product and add it to 1 ml of 40% PEG 400+saline solution, and mix evenly. The mixed solution should be used immediately for optimal results.

* <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	NU1025 (NSC 696807) は、IC50が400 nMの強力なPARP阻害剤です。
in vitro	NU1025 (0.2 mM) treatment attenuates H₂O₂ induced cytotoxicity. This compound per se does not have any effect on cell viability. Its pretreatment significantly increases cell viability (82.59 ?4.67%) in SIN-1 (0.8 mM) exposed cells. It has no detectable effect on the proliferation of D54 and U251 cells. Treatment with this chemical markedly inhibits the enhanced activation of PARP-1 induced by TPT and RT treatment. No DNA strand breakage is detected following exposure to 200 µM of this compound alone.
in vivo	Treatment with NU1025 (1 and 3 mg/kg) reduces the infarction to 25% and 45% versus vehicle treated rats, respectively. This compound (1 and 3 mg/kg) treatment significantly reduces edema volume. It also produces significant improvement in neurological deficits.

プロトコル(参考用のみ)

キナーゼアッセイ	PARP activation assay
キナーゼアッセイ	Cells are suspended in hypotonic buffer (9 mM HEPES, pH 7.8, 4.5% (v/v) dextran, 4.5 mM MgCl₂ and 5 mM DTT) at 1.5 × 107/mL on ice for 30 min, then 9 vol of isotonic buffer (40 mM HEPES, pH 7.8, 130 mM KCl, 4% (v/v) dextran, 2 mM EGTA, 2.3 mM MgCl₂, 225 mM sucrose and 2.5 mM DTT) is added. The reaction is started by adding 300 µL cells to 100 µL 300 µM NAD+ containing [³²P]-NAD+, and terminated by the addition of 2 mL ice-cold 10% (w/v) TCA +10% (w/v) sodium pyrophosphate. After 30 min on ice the precipitated 32P-labelled ADP-ribose polymers are filtered, washed five times with 1% (v/v) TCA, 1% (v/v) sodium pyrophosphate, dried and counted.
細胞アッセイ	細胞株	D54 and U251 cells
	濃度	160 μM
	反応時間	5 days
	実験の流れ	Cells are seeded in 96-well plates at a density of 2,500 cells/well and treated with the indicated doses of NU1025. Adherent cells are irradiated in medium with 250 kVp X-rays (dose rate 0.5 Gy/min). Untreated cells are used as a control. Following an up to 5 day incubation, cell proliferation is assessed by MTT assay.
動物実験	動物モデル	Male Sprague Dawley rats
	投薬量	3 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/16251802/
https://pubmed.ncbi.nlm.nih.gov/16935310/
https://pubmed.ncbi.nlm.nih.gov/25182801/

https://pubmed.ncbi.nlm.nih.gov/11139322/

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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：

DCS, a novel classifier system based on disulfidptosis reveals tumor microenvironment heterogeneity and guides frontline therapy for clear cell renal carcinoma [ J Natl Cancer Cent, 2024, 4(3):263-279]	PubMed: 39281723
Response of Breast Cancer Cells to PARP Inhibitors Is Independent of BRCA Status. [ J Clin Med, 2020, 30;9(4)]	PubMed: 32235451
Effects of Sleep Deprivation (SD) on Rats via ERK1/2 Signaling Pathway. [ Med Sci Monit, 2019, 25:2886-2895]	PubMed: 31002658

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。

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