Tubulin-IN-53
Tubulin-IN-53 is a potent Tubulin inhibitor with an IC50 of 6.06 μM. Tubulin-IN-53 inhibits the polymerization of tubulin by targeting the colchicine binding site of tubulin and destroys the microtubule network. Tubulin-IN-53 induces MCF-7 cell cycle arrest in the G2/M phase and apoptosis, and inhibits cell migration accompanied by the decrease of mitochondrial membrane potential and increase the accumulation of ROS. Tubulin-IN-53 destroys the angiogenesis of human umbilical vein endothelial cells.Tubulin-IN-53 can used for the study of cancers such as breast cancer and lung cancer.
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- Fòrmula: C20H16ClNO6
- Peso molecular:401.80
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
In Vitro
Tubulin-IN-53 (Compound A7) (72 h) exhibits antiproliferative activities in various cancer cells with IC50s of 6, 4, 5, 6, 4 and 10 nM against PC-3, MCF-7, MDA-MB-231, A549, HT-29 and A549/TxR cells and cytotoxicity on normal cells with CC50s of 112 and 220 nM against L02 and MCF-10A cells[1].
Tubulin-IN-53 (5-20 nM, 14 d) consistently inhibits MCF-7 cells colony formation[1].
Tubulin-IN-53 (5-20 nM, 6 h) dose-dependently inhibits the the formation of EBI and β-tubulin adducts and completely disaggregats the microtubule network in MCF-7 cells[1].
Tubulin-IN-53 (5-20 nM, 24 h) induces MCF-7 cell cycle arrest in the G2/M phase and cell apoptosis, and significantly increases intracellular ROS levels[1].
Tubulin-IN-53 (2.5-10 nM, 24 h) inhibits A549 cell migration and effectively inhibits the formation of vascular networks in HUVECs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 cells
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Concentration:5, 10 and 20 nM
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Incubation Time:24 h
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Result:Significantly increased apoptosis rate.
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Cell Line:MCF-7 cells
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Concentration:5, 10 and 20 nM
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Incubation Time:24 h
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Result:Increased the G2/M phase ratio of MCF-7 cells from 18.7% to 76.1%.
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Cell Line:MCF-7 cells
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Concentration:5, 10 and 20 nM
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Incubation Time:24 h
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Result:Upregulated Cyclin B1 expression and reduced Cdc2 phosphorylation (Y15) levels.
Downregulates the anti-apoptotic protein Bcl-2 and upregulates the pro-apoptotic protein Bax.
Increased cleaved PARP and cleaved caspase-3 levels.
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Cell Line:A549 cells
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Concentration:2.5, 5 and 10 nM
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Incubation Time:24 h
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Result:Significantly reduced the number of A549 cells penetrating the membrane.
Significantly inhibited the migration ability of A549 cells.
Chemical Information
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Peso molecular 401.80
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Fòrmula C20H16ClNO6
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SMILES
O=C1OCC2=C1C(C3=CC(OC)=C(OC)C(Cl)=C3)C4=CC5=C(OCO5)C=C4N2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Tubulin-IN-53 Related Classifications
HY-175512 Related Classifications
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