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Purity: ≥98%
SN-38 (NK012; SN-38; NK-012; SN 38; 10-hydroxy-7-ethylcamptothecin) is the active metabolite of Irinotecan (CPT-11) which is a Topoisomerase I inhibitor approved for use as an anticancer drug. SN-38 functions by suppressing DNA synthesis, DNA topoisomerase I, and frequent single-strand breaks in DNA. Its activity is 1000 times greater than that of irinoteca.
| Targets |
Topoisomerase I; Camptothecins
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
In the reaction buffer, which is made up 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, one unit (the minimum amount for full relaxation of 0.5 μg SV40 DNA under the conditions of this study), 0.5 μL of the test compounds, and 0.5μg SV40 DNA are added successively to the reaction buffer. The 50 μL reaction mixture is then incubated for 10 minutes at 37°C. Finally, the reaction is stopped by treating the mixture for 30 more minutes at 37°C with 7.5 μL of a solution that contains 0.5 mg/mL proteinase K, 20 mM EDTA disodium salt, and 1% sodium dodecyl sulfate. The samples are combined with 5 μL of the loading buffer, which has 0.3% bromophenol blue, 31.3% sucrose, and 10 mM NaH2PO4. Form I (supercoiled) and form II (nicked) DNA are separated from relaxed (form Ir) DNA using electrophoresis on an 0.8% agarose gel at 50 mA and 20 V for 17 hours while 2 μg/mL chloroquine, 10 mM EDTA, 30 mM NaH2PO4, and 36 mM Tris-HCl (pH 7.8) are present. Following electrophoresis, 0.05% ethidium bromide staining is applied to the gel, and UV light (302 nm) photography is taken. A densitometer is used to measure the quantity of DNA.
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| Cell Assay |
The MTT assay is used to assess the sensitivity of SN-38 (NK012) in vitro. After seeding cells in 96-well plates, SN-38 (NK012) at various concentrations is added the next day. The medium is discarded after 48 hours of drug exposure, and the plates are then incubated for three hours in medium containing MTT (0.5 mg/mL). The formed formazan is dissolved by adding 20% sodium dodecyl sulphate, which has been acidified (0.02 M HCl). Cell viability is computed as a percentage relative to untreated cells using the optical density at 570 nm (with a background of 670 nm). The mean IC50 value ± standard deviation is found after three iterations of the experiments. The calculation of relative resistance for each resistant cell line involves dividing its mean IC50 value by the mean IC50 value of the corresponding parental cell line.
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| Animal Protocol |
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| References |
| Molecular Formula |
C22H20N2O5
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| Molecular Weight |
392.4
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| Exact Mass |
392.14
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| Elemental Analysis |
C, 67.34; H, 5.14; N, 7.14; O, 20.39
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| CAS # |
86639-52-3
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| Related CAS # |
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| Appearance |
Light yellow solid powder
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| SMILES |
CCC1=C2CN3C(=CC4=C(C3=O)COC(=O)[C@@]4(CC)O)C2=NC5=C1C=C(C=C5)O
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| InChi Key |
FJHBVJOVLFPMQE-QFIPXVFZSA-N
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| InChi Code |
InChI=1S/C22H20N2O5/c1-3-12-13-7-11(25)5-6-17(13)23-19-14(12)9-24-18(19)8-16-15(20(24)26)10-29-21(27)22(16,28)4-2/h5-8,25,28H,3-4,9-10H2,1-2H3/t22-/m0/s1
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| Chemical Name |
(19S)-10,19-diethyl-7,19-dihydroxy-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4(9),5,7,10,15(20)-heptaene-14,18-dione
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.37 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: 2.08 mg/mL (5.30 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: 2.08 mg/mL (5.30 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03785873 | Active Recruiting |
Drug: Nanoliposomal-Irinotecan Drug: Nivolumab |
Biliary Tract Cancer | University of Michigan Rogel Cancer Center |
May 22, 2019 | Phase 1 |
| NCT02138617 | Active Recruiting |
Drug: Irinotecan Drug: Leucovorin |
Colon Cancer | NC Lineberger Comprehensive Cancer Center |
May 2014 | Phase 2 |
| NCT04641871 | Active Recruiting |
Drug: Irinotecan Hydrochloride Drug: Sym023 |
Solid Tumor Metastatic Cancer |
Symphogen A/S | October 12, 2020 | Phase 1 |
| NCT03567629 | Active Recruiting |
Drug: Irinotecan Drug: Oxaliplatin |
mCRC | Peking University | May 29, 2018 | Phase 2 |
| NCT03323034 | Active Recruiting |
Drug: Irinotecan Drug: Pevonedistat |
Recurrent Lymphoma Refractory Lymphoma |
Children's Oncology Group | January 11, 2018 | Phase 1 |
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