Les-6666
Les-6666 is a β-tubulin inhibitor. Les-6666 exerts antiproliferative, pro-apoptotic, cell cycle arrest and migration-inhibitory effects, and suppresses DNA synthesis. Les-6666 can be used in the research of pancreatic cancer.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Formel: C19H14N2O3S
- Molecular Weight:350.39
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
β-Tubulin |
In Vitro
Les-6666 potently inhibits the growth of the NCI-60 human tumor cell line panel with a mean GI50 of 0.056 μM, and shows particularly strong activity against K-562, SR, NCI-H522, and MDA-MB-435 cell lines[1].
Les-6666 (0.001-10 μM; 24-72 h) exhibits potent cytotoxicity against multiple cancer cell lines, with the strongest activity against MIA PaCa-2 pancreatic cancer cells (IC50 = 0.08 μM at 72 h), and shows lower toxicity against normal Beas-2B and HDFa cells[1].
Les-6666 (0.1-1 μM; 48 h) inhibits DNA synthesis and proliferation of MIA PaCa-2 pancreatic cancer cells, reducing [3H]-thymidine incorporation to 35-44% of control levels after 48 h of treatment at 0.1-1 μM[1].
Les-6666 (0.1-1 μM; 48 h) potently suppresses clonogenic survival of MIA PaCa-2 pancreatic cancer cells, reducing the surviving fraction to less than 3% after 48 h of treatment at 0.1-1 μM[1].
Les-6666 (0.1-0.5 μM; 24-48 h) strongly inhibits migration of MIA PaCa-2 pancreatic cancer cells, limiting gap closure to 4.7-10.7% after 24-48 h of treatment at 0.1-0.5 μM[1].
Les-6666 (0.1-0.5 μM; 48 h) induces significant early and late apoptosis in MIA PaCa-2 pancreatic cancer cells, with combined apoptotic populations reaching over 74% after 48 h of treatment at 0.1-0.5 μM[1].
Les-6666 (0.1-0.5 μM; 48 h) arrests MIA PaCa-2 pancreatic cancer cells in the G2/M phase of the cell cycle, increasing the G2/M population to over 33% after 48 h of treatment at 0.1-0.5 μM[1].
Les-6666 (0.1-0.5 μM; 48 h) reduces β-tubulin protein concentration in MIA PaCa-2 pancreatic cancer cells, lowering levels to ~50% of control after 48 h of treatment at 0.1-0.5 μM[1].
Les-6666 (0.1-0.5 μM; 48 h) reduces βIII-tubulin protein expression in MIA PaCa-2 pancreatic cancer cells, lowering levels to 71.7-78.7% of control after 48 h of treatment at 0.1-0.5 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:pancreatic cancer MIA PaCa-2, Capan-2, Panc-1; breast cancer MDA-MB-231, MCF-7, HCC-1954; colon cancer HT-29; gastric cancer AGS; liver cancer HepG2; glioblastoma T98G, U87, A172; lung cancer A549, H1299; normal transformed HDFa, Beas-2B cells
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Concentration:0.001,
0.01, 0.1, 1, 10 μM -
Incubation Time:24 h, 48 h, 72 h
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Result:After 72 h, the IC50 values were 0.08 μM (MIA PaCa-2), 0.71 μM (Capan-2), 5.76 μM (Panc-1), 1.26 μM (HCC-1954), 0.86 μM (HT-29), 1.82 μM (T98G), 0.45 μM (A549), > 10 μM (MDA-MB-231, MCF-7, AGS, HepG2, U87, A172, H1299), > 10 μM (HDFa), and 1.10 μM (Beas-2B).
After 24 h, the IC50 for MIA PaCa-2 was 5.73 μM; after 48 h, it was 0.48 μM.
The IC50 for Beas-2B after 48 h was 3.89 μM, and no measurable IC50 was observed for HDFa after 48 h.
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Cell Line:pancreatic cancer MIA PaCa-2 cells
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Concentration:0.1, 0.5 and 1 μM
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Incubation Time:48 h
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Result:At 0.1 μM, [3H]-thymidine incorporation was 41.00% relative to control; at 0.5 μM, it was 44.33% relative to control; at 1 μM, it was 35.00% relative to control.
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Cell Line:pancreatic cancer MIA PaCa-2 cells
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Concentration:0.1, 0.5 and 1 μM
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Incubation Time:24 h, 48 h, 72 h
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Result:After 48 h of treatment at all tested concentrations, the surviving fraction was reduced to less than 3% relative to control.
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Cell Line:pancreatic cancer MIA PaCa-2 cells
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Concentration:0.1, 0.5 and 1 μM
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Incubation Time:24 h, 48 h
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Result:At 24 h, gap closure was 4.7% (0.5 μM) and 6.3% (0.1 μM) relative to 40% in control; at 48 h, gap closure was 8.3% (0.5 μM) and 10.7% (0.1 μM) relative to 57% in control.
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Cell Line:pancreatic cancer MIA PaCa-2 cells
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Concentration:0.1, 0.5 and 1 μM
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Incubation Time:48 h
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Result:At 0.1 μM, early apoptosis was 20.40% and late apoptosis was 54.37% relative to 4.37% early and 15.67% late apoptosis in control; at 0.5 μM, early apoptosis was 20.93% and late apoptosis was 53.43% relative to control.
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Cell Line:pancreatic cancer MIA PaCa-2 cells
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Concentration:0.1, 0.5 and 1 μM
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Incubation Time:48 h
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Result:At both 0.1 μM and 0.5 μM, over 33% of cells were arrested in the G2/M phase, compared to 22.17% in control.
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Cell Line:pancreatic cancer MIA PaCa-2 cells
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Concentration:0.1, 0.5 and 1 μM
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Incubation Time:48 h
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Result:At 0.1 μM, β-tubulin concentration was 648.3 pg/mL; at 0.5 μM, it was 640.4 pg/mL, compared to 1289.0 pg/mL in control.
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Cell Line:pancreatic cancer MIA PaCa-2 cells
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Concentration:0.1, 0.5 and 1 μM
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Incubation Time:48 h
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Result:At 0.1 μM, relative βIII-tubulin expression was 78.7% of control; at 0.5 μM, it was 71.7% of control.
Chemical Information
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Molecular Weight 350.39
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Formel C19H14N2O3S
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SMILES
OC(C=C1)=CC=C1NC(S/2)=NC(C2=C\C3=CC=CC=C3OCC#C)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Les-6666 Related Classifications
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