Tubulin-IN-63
Tubulin-IN-63 is a potent tubulin polymerization inhibitor targeting the colchicine-binding site, with an IC50 of 6.03 µM. Tubulin-IN-63 disrupts microtubule dynamics, induces G2/M arrest and apoptosis, thereby suppressing cancer cell proliferation. Tubulin-IN-63 disrupts capillary network formation in human umbilical vein endothelial cells (HUVECs) and exhibits in vivo antitumor efficacy in a B16-F10 mouse model. Tubulin-IN-63 can be used for the research of cancers, such as melanoma, lung cancer, and liver cancer.
For research use only. We do not sell to patients.
- Formula: C26H23N3O3
- Molecular Weight:425.48
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Tubulin-IN-63 (compound 4a) (48 h) demonstrates potent antiproliferative activity against multiple cancer cell lines (B16-F10, MCF-7, Hela, and HepG-2) with IC50s of 0.052, 0.045, 0.076, and 0.036 µM, respectively, while showing low cytotoxicity in normal cell lines (HUVECs, MCF-10A, and LO2) with IC50s of 751, 903, and 579 nM, respectively, indicating its selectivity[1].
Tubulin-IN-63 (48 h) inhibits the proliferation of A549 and A2780 cells with IC50s of 85.3 and 42.4 nM, and retains efficacy against Paclitaxel (HY-B0015)-resistant cells (A549/T and A2780/T cells) with IC50s of 172.5 and 61.8 nM, indicating its capacity to circumvent Paclitaxel-associated drug resistance[1].
Tubulin-IN-63 (10-100 nM, 24 h) exerts durable inhibition of cancer cell growth and proliferation in HepG-2 cells, as evidenced by a dose-dependent reduction in clonogenic survival after 10-14 days of drug-free culture[1].
Tubulin-IN-63 (10-100 nM, 48 h) induces G2/M phase cell cycle arrest and apoptosis in HepG-2 cells in a dose-dependent manner[1].
Tubulin-IN-63 (10-100 nM, 0-24 h) inhibits HepG-2 cell migration in a concentration-dependent manner[1].
Tubulin-IN-63 (10-100 nM, 12 h) induces dose-dependent microtubule network disruption in HepG-2 cells[1].
Tubulin-IN-63 (10-100 nM, 6 h) disrupts vascular network formation 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:HepG-2
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Concentration:10, 50, 100 nM
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Incubation Time:24 h
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Result:Dose-dependently restrained colony formation.
Almost completely abolished the clonogenic capacity of HepG-2 cells at 50 nM.
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Cell Line:HepG-2
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Concentration:10, 50, 100 nM
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Incubation Time:48 h
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Result:Caused a dose-dependent G2/M phase arrest in HepG-2 cells, with the percentage of cells in G2/M increasing from 15.6% to 33.8%.
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Cell Line:HepG-2
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Concentration:10, 50, 100 nM
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Incubation Time:48 h
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Result:Caused a dose-dependent increase in apoptosis in HepG-2 cells, with total apoptotic cell percentages of 18.02%, 42.90%, and 53.73% at 10, 50, and 100 nM, respectively.
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Cell Line:HepG-2
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Concentration:10, 50, 100 nM
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Incubation Time:0, 24 h
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Result:Dose-dependently inhibited the migration of HepG-2 cells, with the recovered area decreasing to 35.41% at 10 nM, 20.69% at 50 nM, and 13.91% at 100 nM.
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Cell Line:HUVECs
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Concentration:10, 50, 100 nM
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Incubation Time:6 h
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Result:Dose-dependently disrupted the formation of capillary-like networks in HUVECs.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 mice subcutaneously injected with B16-F10 cells[1]
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Dosage:10 mg/kg
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Administration:i.p., daily for 14 days
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Result:Significantly suppressed tumor growth, achieving a TGI value of 69.25%.
Resulted in a pronounced synergistic antitumor effect, when combined with NP19 (5 mg/kg), with a TGI of 85.20%.
Showed no significant toxicity in vital organs (heart, liver, and kidney).
Chemical Information
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Molecular Weight 425.48
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Formula C26H23N3O3
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SMILES
CN1C=CC2=C1C=CC(C3=CC=C4N=CN=C(C5=CC(OC)=C(OC)C(OC)=C5)C4=C3)=C2
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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)