SN-38

製品コードS4908 バッチS490805

印刷

化学情報

Chemical Structure Synonyms NK012 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C22H20N2O5
分子量 392.4 CAS No. 86639-52-3
Solubility (25°C)* 体外 DMSO 20 mg/mL (50.96 mM)
Water Insoluble
Ethanol 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 40%PEG300 5%Tween80 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。

 0.630mg/ml (1.61mM) Taking the 1 mL working solution as an example, add 50 μL of 12.5 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 make it clear. Volume up to 1 mL. 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 SN-38 (NK012) is an active metabolite of CPT-11, inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks. SN-38 induces autophagy.
in vitro

SN-38, a biological active metabolite of  CPT-11. This compound causes the strongest inhibition of DNA topoisomerase I, followed by CPT and then CPT-11. CPT-11 dose dependently shifts the position of relaxed DNA in the direction of nicked DNA, but this compound and CPT shows no effect on the position of relaxed DNA. It dose-dependently and time-dependently inhibit DNA synthesis. Respective IC50 values of this chemical, in DNA synthesis is 0.077 μM. The inhibitory effect of it on RNA synthesis is less than that on DNA synthesis and it does not inhibit protein synthesis. This metabolite caused frequent DNA single-strand breaks in P388 cells. [1]
in vivo

After oral dosing, peak concentrations of this compound occur within 1 h, and the percent unbound lactone in murine plasma at 1000 ng/mL is 3.4 +/- 0.67%, whereas at 100 ng/mL the percent unbound is 1.18 +/- 0.14%. Lactone AUCs in mice bearing human neuroblastoma xenografts are greater than in nontumor-bearing animals. [2]

プロトコル(参考用のみ)

キナーゼアッセイ Topoisomerase I Assay
One unit (the minimum amount for full relaxation of 0.5 μg SV40 DNA under the conditions of this study) of topoisomerase I, 0.5 μL of the test compounds, and 0.5μg SV40 DNA are added sequentially to the reaction buffer, which is composed of 25 mM Tris-HCl (pH 7.5), 50 mM KC1, 5 mM MgCl2, 0.25 mM EDTA disodium salt, 0.25 mM dithiothreitol, 15μg /mL bovine serum albumin, and 5% glycerol. Then, the reaction mixture (50 μL) is incubated for 10 min at 37 °C, and the reaction is terminated by treatment with 7.5 μL of a solution consisting of 1% sodium dodecyl sulfate, 20 mM EDTA disodium salt, and 0.5 mg/mL proteinase K for an additional 30 min at 37°C. The samples are mixed with 5 μL of the loading buffer containing 10 mM Na2HPO4, 31.3% sucrose, and 0.3% bromophenol blue. Relaxed (form Ir) DNA is separated from supercoiled (form I) and nicked (form II) DNA by electrophoresis on 0.8% agarose gel at 50 mA and 20 V for 17 h in the presence of 2 μg/mL CHQ, 10 mM EDTA, 30 mM NaH2PO4, and 36 Mm Tris-HCl (pH 7.8). After electrophoresis, the gel is stained with 0.05% ethidium bromide and photographed with UV light (302 nm). The amount of DNA is quantified using a densitometer.
細胞アッセイ 細胞株 A-172, U-87, and LA-567
濃度 0 -1000 nM
反応時間 48 h
実験の流れ

MTT assay
動物実験 動物モデル Male Sprague-Dawley rats
投薬量 10 mg/kg
投与方法 i.v.

参考

  • https://pubmed.ncbi.nlm.nih.gov/1651156/
  • http://www.ncbi.nlm.nih.gov/pubmed/ 9219511
  • https://pubmed.ncbi.nlm.nih.gov/12712458/
  • https://pubmed.ncbi.nlm.nih.gov/30587986/

カスタマーフィードバック

Data from [J Pharmacol Exp Ther, 2014, 348(3), 432-41]

Data from [Data independently produced by , , J Control Release, 2018, 275:85-91]

Data from [Data independently produced by , , Cancer Lett, 2017, 411:35-43]

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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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