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SN-38

Catalog No. T1703 CAS 86639-52-3

Synonyms: NK012, SN 38

SN-38 (NK012) is the active metabolite of Irinotecan, a DNA topoisomerase I (Topo I) inhibitor, which inhibits DNA and RNA synthesis (IC50=0.077/1.3 μM). SN-38 has antitumor activity and induces autophagy.

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SN-38, CAS 86639-52-3

Pack Size	Availability	Price/USD
25 mg	In stock	$ 39.00
50 mg	In stock	$ 55.00
100 mg	In stock	$ 77.00
500 mg	In stock	$ 150.00
1 mL * 10 mM (in DMSO)	In stock	$ 61.00

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Purity: 99.97%

Purity: 99.95%

Purity: 99.6%

Purity: 98%

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Description	SN-38 (NK012) is the active metabolite of Irinotecan, a DNA topoisomerase I (Topo I) inhibitor, which inhibits DNA and RNA synthesis (IC50=0.077/1.3 μM). SN-38 has antitumor activity and induces autophagy.
Targets&IC50	DNA synthesis:0.077 μM, RNA synthesis:1.3 μM
In vitro	METHODS: Lung cancer cells LLC, A549 and H358 were treated with SN-38 (10-1000 nM) for 48 h. Cell viability was detected using MTT assay. RESULTS: SN-38 started to exhibit effects at 10 nM concentration and induced about 50% cell death at 100 nM. [1] METHODS: Colorectal cancer cells KM12C, KM12SM and KM12L4a were treated with SN-38 (2.5 µg/mL) for 4-48 h. Cell cycle and apoptosis were detected by Flow cytometry. RESULTS: SN-38 induced S-phase and G2-phase block, with KM12L4a cells responding most strongly in a time-dependent manner. apoptosis increased over time in the KM12SM and KM12L4a cell lines, but there was no such change in the KM12C cells. [2]
In vivo	METHODS: To test the antitumor activity in vivo, SN-38 (2 mg/kg) was administered by single intraperitoneal injection to C57BL/6 mice transplanted with LLC cells in the peritoneal cavity. RESULTS: A single intraperitoneal injection of SN-38 significantly attenuated the growth of LLC tumors, resulting in a 22.7% reduction in tumor growth. [1] METHODS: To test the antitumor activity in vivo, SN-38 (10 mg/kg in 0.5% carboxymethylcellulose sodium, intraperitoneal injection) and gefitinib (100 mg/kg, subcutaneous injection) were administered to BALB/c nude mice bearing human oral squamous tumors HSC-2 five times per week for three weeks. RESULTS: Only gefitinib was administered to mice with human oral squamous tumors. RESULTS: There was no significant difference in tumor growth inhibition between gefitinib only and gefitinib plus SN-38 treatment. However, some tumors in the gefitinib-only group showed new growth when tumor measurements were continued after treatment was stopped. [3]
Kinase Assay	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 chloroquine, 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.
Cell Research	MTT assay(Only for Reference)
Source	Natural Products > Nyssaceae > Camptotheca

Synonyms	NK012, SN 38
Molecular Weight	392.4
Formula	C22H20N2O5
CAS No.	86639-52-3

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 39.2 mg/mL (100 mM)

References and Literature

1. Maurya DK, et al. Topoisomerase I inhibitor SN-38 effectively attenuates growth of human non-small cell lung cancer cell lines in vitro and in vivo. J Environ Pathol Toxicol Oncol. 2011;30(1):1-10. 2. Wallin A, et al. Anticancer effect of SN-38 on colon cancer cell lines with different metastatic potential. Oncol Rep. 2008 Jun;19(6):1493-8. 3. Nanbu T, et al. Combined SN-38 and gefitinib treatment promotes CD44 degradation in head and neck squamous cell carcinoma cells. Oncol Rep. 2018 Jan;39(1):367-375.

Citations

1. Boos S L, Loevenich L P, Vosberg S, et al Disease Modeling on Tumor Organoids Implicates AURKA as a Therapeutic Target in Liver Metastatic Colorectal Cancer. Cellular and Molecular Gastroenterology and Hepatology. 2021 2. Larson T S, Glish G L, Lockett M R. Spatially resolved quantification of drug metabolism and efficacy in 3D paper-based tumor mimics. Analytica Chimica Acta. 2021: 339091.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Clinical Compound Library Immunology/Inflammation Compound Library Anti-Aging Compound Library Anti-Colorectal Cancer Traditional Chinese Medicine Compound Library Anti-Tumor Natural Product Library Bioactive Compound Library

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Keywords

SN-38 86639-52-3 Autophagy Cell Cycle/Checkpoint DNA Damage/DNA Repair DNA/RNA Synthesis Topoisomerase inhibit NK 012 NK012 Inhibitor ADC Cytotoxin SN38 SN 38 ADC Payload NK-012 inhibitor

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