1. Cell Cycle/DNA Damage
    Antibody-drug Conjugate/ADC Related
    Autophagy
  2. Topoisomerase
    ADC Cytotoxin
    Autophagy
  3. SN-38

SN-38 (Synonyms: NK012)

製品番号: HY-13704 純度: 99.46%
取扱説明書

SN-38 (NK012) is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively.

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SN-38 構造式

SN-38 構造式

CAS 番号 : 86639-52-3

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
10 mM * 1 mL in DMSO USD 77 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 70 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 96 在庫あり
Estimated Time of Arrival: December 31
200 mg USD 180 在庫あり
Estimated Time of Arrival: December 31
500 mg USD 288 在庫あり
Estimated Time of Arrival: December 31
1 g   お問い合わせ  
5 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 10 publication(s) in Google Scholar

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製品説明

SN-38 (NK012) is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively.

IC50 & Target[1]

Topoisomerase I

 

Camptothecins

 

体外実験

The IC50 values for LoVo, HCT116, and HT29 cell lines is 20 nM, 50 nM, 130 nM, respectively. In all three SN-38 (NK012) resistant cell lines Top1 activity is maintained in the presence of high concentrations of SN-38[2].

体内実験

SN-38 (NK012), the active and toxic metabolite of the anticancer prodrug Irinotecan. At 30 minutes after administration, Irinotecan plasma concentrations in Slco1a/1b(−/−) mice are 1.9-fold higher than in the wild-type mice (1.89 vs. 1.01 μM, respectively), whereas SN-38 (NK012) plasma concentrations of Slco1a/1b(−/−) mice are 8-fold higher compare with wild-type mice (0.4 μg/mL vs. 0.05 μg/mL, respectively). Overall plasma exposure [AUC(5-240)] of Irinotecan is 1.7-fold higher in Oatp1a/1b knockout mice versus wild-type mice (209.8±6.7 vs. 120.9±4.4 μM/min; P<0.01), and 2.9-fold higher for SN-38 (50±2.9 vs. 12±2 μM/min; P<0.001)[3].

臨床実験
分子量

392.40

分子式

C₂₂H₂₀N₂O₅

CAS 番号

86639-52-3

SMILES

O=C1[[email protected]](O)(CC)C2=C(CO1)C(N3CC4=C(CC)C5=CC(O)=CC=C5N=C4C3=C2)=O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 25 mg/mL (63.71 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5484 mL 12.7421 mL 25.4842 mL
5 mM 0.5097 mL 2.5484 mL 5.0968 mL
10 mM 0.2548 mL 1.2742 mL 2.5484 mL
*Please refer to the solubility information to select the appropriate solvent.
体内:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (6.37 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (6.37 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: 2.5 mg/mL (6.37 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
参考文献
細胞実験
[2]

In vitro SN-38 (NK012) sensitivity is determined using the MTT assay. Cells are seeded in 96-well plates, and a range of SN-38 (NK012) concentrations is added the following day. Following 48 h of drug exposure, the medium is discarded and the plates are incubated with medium containing MTT (0.5 mg/mL) for 3 h. Acidified (0.02 M HCl) sodium dodecyl sulphate (20 %) is added to dissolve the formed formazan. Optical density at 570 nm (and 670 nm for background) is measured, and the cell viability is calculated in percent compared to untreated cells. Experiments are repeated three times and the mean IC50 value ± standard deviation is determined. Relative resistance for each resistant cell line is calculated by dividing the mean IC50 value of the resistant cell line by the mean IC50 value of the corresponding parental cell line[2].

MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

動物実験
[3]

Mice[3]
Female wild-type, Slco1a/1b(−/−)(Oatp1a/1b knockout), Slco1a/1b(−/−);1B1(tg), and Slco1a/1b(−/−);1B3(tg) (liver-specific OATP1B1 and OATP1B3 humanized transgenic) mice of comparable genetic background (>99% FVB) between 8 and 14 weeks of age are used. Irinotecan (20 mg/mL in water-based solution containing NaOH, lactic acid, and sorbitol) is diluted with saline (to 2 mg/mL) for administration of 10 mg/kg; 5 μL/g bodyweight are administered intravenously to mice. SN-38 (NK012) is dissolved in DMSO (1 mg/mL) and 1 μL/g body weight is administered intravenously to mice to achieve a dosage of 1 mg/kg. The experiments are terminated by isoflurane anaesthesia, heparin-blood sampling by cardiac puncture followed by cervical dislocation and tissue collection. Blood samples are centrifuged at 5,200 × g for 5 minutes at 4°C and plasma is collected and stored at −30°C until analysis.

MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

参考文献

純度: 99.46%

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Keywords:

SN-38NK012SN38SN 38NK 012NK-012TopoisomeraseADC CytotoxinAutophagyInhibitorinhibitorinhibit

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SN-38
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