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SN-38

SKU: orb1307686

Description

SN-38 (NK012) is the active metabolite of the Topoisomerase I inhibitor Irinotecan. It potently inhibits DNA/RNA synthesis and exhibits antitumor activity, including the induction of autophagy, making it a valuable tool for in vitro and in vivo cancer research.

Research Area

Cell Biology, Metabolism Research, Molecular Biology

Images & Validation

Key Properties

CAS Number86639-52-3
MW392.41
Purity>98%
FormulaC22H20N2O5
SMILESC(C)C1=C2C(C=3N(C2)C(=O)C4=C(C3)[C@](CC)(O)C(=O)OC4)=NC=5C1=CC(O)=CC5
TargetTopoisomerase
SolubilitySoluble in DMSO (up to 40 mg/ml).

Bioactivity

Target IC50
RNA synthesis:1.3 μM|CLM22 organoids:10.67 nM|A549 cells proliferation:200.0 ± 14.9 ng/mL|CWH22 organoids:7.54 nM|MCF-7 cells proliferation:16.0 ± 0.7 ng/mL|DNA synthesis:0.077 μM
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. 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.
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. 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.
Cell Research
MTT assay(Only for Reference)

Storage & Handling

Storage-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

ADC Payload, ADC Cytotoxin, ADCCytotoxin, Autophagy, DNA synthesis, DNA Synthesis, DNASynthesis, Inhibitor, inhibit, NK012, NK-012, NK 012, Topoisomerase, Topo I, RNA Synthesis, RNASynthesis, SN 38, SN38, SN-38

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Key Properties

No computed properties available.

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SN-38 (orb1307686)

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% DMSO +
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% Tween 80 +
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10 mg
$ 210.00
50 mg
$ 480.00
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