Tubulin-IN-66
Tubulin-IN-66 is a tubulin (tubulin) and P-gp inhibitor with antiproliferative activity against cancer cells. Tubulin-IN-66 covalently binds to the Colchicine (HY-16569)-binding site at Cys239 of the β-tubulin subunit, inhibits tubulin polymerization and disrupts the microtubule network. Tubulin-IN-66 inhibits P-gp function to overcome multidrug resistance. Tubulin-IN-66 arrests the cell cycle at the G2/M phase and induces apoptosis (apoptosis). Tubulin-IN-66 inhibits colony formation and migration of cancer cells. Tubulin-IN-66 can be used in the research of tumors such as breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 3110538-32-1
- Formula: C22H24N2O6
- Molecular Weight:412.44
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Tubulin-IN-66 (compound 10v) (48 h) potently inhibits the proliferation of HT-1080, MCF-7 and MDA-MB-231 cancer cells, with IC50 values of 0.30 μM, 0.24 μM and 0.48 μM, respectively[1].
Tubulin-IN-66 (50-200 nM; 8 days) potently inhibits colony formation of HT-1080 and MCF-7 cells in a concentration-dependent manner[1].
Tubulin-IN-66 (150-350 nM; 4-12 h) potently inhibits the migratory capacity of HT-1080 cells in a concentration-dependent manner[1].
Tubulin-IN-66 (5-30 μM; 90 min) inhibits the polymerization of purified tubulin in a concentration-dependent manner[1].
Tubulin-IN-66 (150-450 nM; 24 h) induces concentration-dependent G2/M cell cycle arrest in HT-1080 cells, accompanied by upregulated expression of Cyclin B1, CDK1 and p-H3[1].
Tubulin-IN-66 (150-450 nM; 48 h) induces early apoptosis in HT-1080 cells in a concentration-dependent manner, and its mechanism involves the upregulation of Bax expression and the downregulation of Bcl-2 expression[1].
Tubulin-IN-66 (150-450 nM; 48 h) reduces the mitochondrial membrane potential of HT-1080 cells in a concentration-dependent manner[1].
Tubulin-IN-66 (48 h) potently inhibits the proliferation of doxorubicin-resistant MCF-7/ADM cells, with an IC50 of 0.30 μM after 48 h of treatment. Its resistance index is 1.25, indicating extremely low drug resistance[1].
Tubulin-IN-66 (5-10 μM; 15 min) inhibits the function of P-gp in MCF-7/ADM cells[1].
Tubulin-IN-66 (48 h) exhibits cytotoxicity against human normal cells HUVEC and 293T, with IC50 values of 0.64 μM and 0.34 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT-1080 fibrosarcoma cells, MCF-7 breast cancer cells
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Concentration:50, 100, 200 nM
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Incubation Time:8 days
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Result:Inhibited colony formation in both cell lines in a concentration-dependent manner, with near-complete inhibition observed at the highest tested concentration.
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Cell Line:HT-1080 fibrosarcoma cells
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Concentration:150, 300, 450 nM
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Incubation Time:24 h
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Result:Induced concentration-dependent G2/M phase cell cycle arrest, with a corresponding reduction in G0/G1 phase cell proportion.
Upregulated Cyclin B1, CDK1, and p-H3 protein expression in a concentration-dependent manner via Western blot.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice treated 4T1 cells (female, 6-8 weeks of age)[1]
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Dosage:10 mg/kg; 20 mg/kg; 50 mg/kg
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Administration:i.p.; every other day; 14 days
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Result:Showed no significant intergroup differences in mouse body weight, with no observable adverse effects.
Significantly decreased tumor volume and weight in a dose-dependent manner, with tumor growth inhibition (TGI) values of 46.76% (10 mg/kg), 53.96% (20 mg/kg), and 64.51% (50 mg/kg).
Exhibited no obvious pathological injury in major organs (heart, liver, spleen, lung, kidney) via hematoxylin and eosin (H&E) staining.
Chemical Information
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CAS No. 3110538-32-1
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Molecular Weight 412.44
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Formula C22H24N2O6
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SMILES
COC(C1=CC2=C(N(CCN2)C(/C=C/C3=CC(OC)=C(C(OC)=C3)OC)=O)C=C1)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Tubulin-IN-66 Related Classifications
HY-182753 Related Classifications
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