1. Cell Cycle/DNA Damage
    Autophagy
  2. Topoisomerase
    Autophagy

SN-38 (Synonyms: NK012)

Cat. No.: HY-13704 Purity: 99.46%
Handling Instructions

SN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan.

For research use only. We do not sell to patients.

SN-38 Chemical Structure

SN-38 Chemical Structure

CAS No. : 86639-52-3

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 106 In-stock
Estimated Time of Arrival: December 31
100 mg USD 96 In-stock
Estimated Time of Arrival: December 31
200 mg USD 180 In-stock
Estimated Time of Arrival: December 31
500 mg USD 288 In-stock
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

SN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan.

IC50 & Target[1]

Topoisomerase I

 

In Vitro

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

In Vivo

SN-38, 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 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].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : ≥ 40 mg/mL (101.94 mM)

*"≥" means soluble, but saturation unknown.

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.
References
Kinase Assay
[2]

LoVo, HCT116, and HT29 cell lines are trypsinized, resuspended and counted, and for each cell line 1 million cells are pipetted to each of three eppendorf tubes on ice. Cells are pelleted (5 min centrifugation, 300 g, 4°C) and snap-frozen in dry ice and ethanol and stored at -80°C until analysis. Nuclear extracts are prepared essentially, and Top1 activity measured in titration experiments with or without added SN-38 (at concentrations stated in the text) using the standard Rolling circle Enhanced Enzyme Activity Detection (REEAD) protocol. The activity is calculated in terms of numbers of Top1 specific signals relative to the amount of signals resulting from the addition a known concentration of control circles[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[2]

In vitro SN-38 sensitivity is determined using the MTT assay. Cells are seeded in 96-well plates, and a range of SN-38 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 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[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 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 has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

392.40

Formula

C₂₂H₂₀N₂O₅

CAS No.

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.46%

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SN-38
Cat. No.:
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SN-38

Cat. No.: HY-13704