Beta-Lapachone

製品コードS7261 バッチS726102

印刷

化学情報

Synonyms

β-Lapachone, ARQ-501

Storage
(From the date of receipt)

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

化学式

C₁₅H₁₄O₃

分子量

242.27

CAS No.

4707-32-8

Solubility (25°C)*

体外

DMSO (warmed with 50ºC water bath)

33 mg/mL (136.21 mM)

Ethanol

16 mg/mL (66.04 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	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O 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。	2.000mg/ml (8.26mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil 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。	2.000mg/ml (8.26mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clear DMSO stock solution to 950 μL of corn oil 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	Beta-Lapachone (β-Lapachone、ARQ-501) は、DNAトポイソメラーゼIIまたはリガーゼに対して阻害活性を示さない、選択的なDNAトポイソメラーゼI阻害剤です。フェーズ2。
in vitro	Beta-Lapachone inhibits DNA relaxation induced by DNA topoisomerase I in a dose-dependent manner. Treatment of this compound (100 nM or greater) results in >95% inhibition of Topo I DNA unwinding activity compared to the DMSO control. This chemical (1-5 μM) causes a block in G0/G1 of the cell cycle and induces apoptosis by locking Topo I onto DNA and blocking replication fork movement in HL-60 and three human prostate cancer (DU-145, PC-3, and LNCaP) cells. It facilitates the migration of mouse 3T3 fibroblasts and human endothelial EAhy926 cells through different MAPK signaling pathways, and thus accelerates scrape-wound healing in vitro. In addition, this compound inhibits purified recombinant IDO1 activity through uncompetitive inhibition with IC50 of 0.44 μM, and it also exhibits superior retention of intracellular IDO1 inhibitory activity with an IC50 of 1.0 μM, partially dependent on biotransformation by NQO1. This chemical induces programmed necrosis of NQO1+ cancer cells by NQO1-dependent reactive oxygen species (ROS) formation and PARP1 hyperactivation. [5]
in vivo	Beta-lapachone treatment (50 mg/kg) leads to potent inhibition of in vivo tumor growth in a xenograft mouse model of human ovarian cancer, and the combination of this compound and taxol produces a synergistic induction of apoptosis. In normal and diabetic (db/db) mice, treatment of this chemical results in a faster healing process than vehicle only.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HL-60, PC-3, DU145, and LNCaP cells
	濃度	0.005 to 50 μM
	反応時間	12 hours
	実験の流れ	IC50 calculations for each cell line are determined by DNA amount (IS) and anchorage-dependent colony formation (CF) assays. For the CF assay, cells are seeded at 500 viable cells/well in 6-well plates and incubated overnight, then treated with equal volumes of media containing beta-lapachone at final concentrations ranging from 0.005 to 50 μM in half-log increments (controls were treated with 0.25% DMSO, equivalent to the highest dose of this compound used) for 4 hour or for continuous 12-hour exposures. Plates (3 wells/condition) are stained with crystal violet, and colonies of >50 normal-appearing cells are enumerated. IC50 values for various cells are calculated using drug doses with numbers of colonies surrounding 50% of control. For DNA assays, plates are harvested for IC50 determinations 8 days after treatment using a CytoFluor 2350 fluorescence measurement system. Six-well samplings are included in the calculation of DNA fluor units for each dose. A graph of this chemical dose versus percentage control DNA in fluor units is used to calculate each IC50. All experiments are repeated at least twice, each in duplicate.
動物実験	動物モデル	Human ovarian cancer cells (36M2) are established in nude mice.
	投薬量	25–50 mg/kg
	投与方法	Intraperitoneal administration

参考

https://pubmed.ncbi.nlm.nih.gov/8226754/
https://pubmed.ncbi.nlm.nih.gov/7641180/
https://pubmed.ncbi.nlm.nih.gov/18650264/

https://pubmed.ncbi.nlm.nih.gov/24023520/
https://pubmed.ncbi.nlm.nih.gov/22532167/
https://pubmed.ncbi.nlm.nih.gov/10557327/

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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：

Visualization strategies to aid interpretation of high-dimensional genotoxicity data [ Environ Mol Mutagen, 2024, 10.1002/em.22604]	PubMed: 38757760
High‑throughput screening identification of a small‑molecule compound that induces ferroptosis and attenuates the invasion and migration of hepatocellular carcinoma cells by targeting the STAT3/GPX4 axis [ Int J Oncol, 2023, 62(3)42]	PubMed: 36825585
Characterizing Mechanisms of Potential Inhibitors of the Hsp90 Chaperone Complex [ ProQuest , 2023, 30489399]	PubMed: None
Potential drug discovery for COVID-19 treatment targeting Cathepsin L using a deep learning-based strategy [ Comput Struct Biotechnol J, 2022, 20:2442-2454]	PubMed: 35602976
Receptor-interacting serine/threonine-protein kinase 1 (RIPK1) inhibitors Necrostatin-1 (Nec-1) and 7-Cl-O-Nec-1 (Nec-1s) are potent inhibitors of NAD(P)H: Quinone oxidoreductase 1 (NQO1) [ Free Radic Biol Med, 2021, 173:64-69]	PubMed: 34252539
CD38 Drives Progress of Osteoarthritis by Affecting Cartilage Homeostasis [ Front Pharmacol, 2021, 12:766909]	PubMed: 34790130
Kinetics of γH2AX and phospho-histone H3 following pulse treatment of TK6 cells provides insights into clastogenic activity [ Mutagenesis, 2021, geab014]	PubMed: 33964157
Nitazoxanide, an anti-parasitic drug, efficiently ameliorates learning and memory impairments in AD model mice. [ Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0220-1]	PubMed: 31000769
Predictions of genotoxic potential, mode of action, molecular targets, and potency via a tiered multiflow® assay data analysis strategy [ Environ Mol Mutagen, 2019, 60(6):513-533]	PubMed: 30702769
Peroxiredoxin V Reduces β-Lapachone-induced Apoptosis of Colon Cancer Cells. [ Anticancer Res, 2019, 39(7):3677-3686]	PubMed: 31262894

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。