Tubulin-IN-67
Tubulin-IN-67 is a tubulin inhibitor. Tubulin-IN-67 binds to the colchicine-binding site of tubulin, inhibiting tubulin polymerization. Tubulin-IN-67 arrests cancer cell cycle at the G2/M phase and triggers apoptosis in cancer cells. Tubulin-IN-67 can be used for the research of hepatocellular carcinoma, cervical carcinoma, breast carcinoma.
For research use only. We do not sell to patients.
- Formula: C23H20N4O3
- Molecular Weight:400.43
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vitro
Tubulin-IN-67 (Compound 15u) (72 h) potently inhibits the proliferation of Huh7, HeLa, and MCF-7 cancer cells with IC50 values of 0.090 μM, 0.10 μM and 0.12 μM, respectively, and displays a markedly improved safety window relative to CA-4 in normal HUVECs[1].
Tubulin-IN-67 (0.5-1 μM) functions as a direct microtubule-destabilizing compound that potently inhibits purified tubulin polymerization in vitro[1].
Tubulin-IN-67 (90-180 nM; 24 h) disrupts the intracellular microtubule network in Huh7 cells, inducing perinuclear microtubule condensation consistent with colchicine-site tubulin inhibition[1].
Tubulin-IN-67 (90-270 nM; 24 h) induces robust, dose-dependent G2/M phase cell cycle arrest in Huh7 cells, with the highest tested concentration (270 nM) resulting in 83.16% of cells arrested in G2/M[1].
Tubulin-IN-67 (90-270 nM; 48 h) effectively induces dose-dependent apoptosis in Huh7 cells, reaching a total apoptotic rate of 46.6% at the highest tested concentration of 270 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Huh7 human hepatocellular carcinoma cells
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Concentration:90 nM; 180 nM
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Incubation Time:24 h
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Result:Induced pronounced morphological alterations to the microtubule cytoskeleton, causing microtubules to become shortened and condensed in a perinuclear localization, similar to the effect of the colchicine-site binder CA-4 (90 nM).
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Cell Line:Huh7 human hepatocellular carcinoma cells
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Concentration:90 nM; 180 nM; 270 nM
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Incubation Time:24 h
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Result:Caused a dose-dependent accumulation of cells in the G2/M phase, increasing the proportion from 4.0% in untreated controls to 13.69% (90 nM), 69.46% (180 nM), and 83.16% (270 nM).
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Cell Line:Huh7 human hepatocellular carcinoma cells
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Concentration:90 nM; 180 nM; 270 nM
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Incubation Time:48 h
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Result:Triggered apoptosis in a concentration-dependent manner, with total apoptotic rates (early + late) of 15.5% (90 nM), 27.0% (180 nM), and 46.6% (270 nM).
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (male, 5 weeks old, specific pathogen-free; orthotopic hepatocellular carcinoma model via Huh7 cell surgical implantation)[1]
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Dosage:15 mg/kg
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Administration:i.p.; every other day; 14 days
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Result:Induced significant tumor progression inhibition relative to vehicle control, with efficacy comparable to Paclitaxel.
Maintained stable body weights without notable decline.
Showed intact liver tissue architecture with no signs of hepatocellular damage or inflammatory infiltration, while tumor sections exhibited extensive necrotic regions exceeding those in the vehicle group.
Chemical Information
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Molecular Weight 400.43
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Formula C23H20N4O3
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SMILES
COC1=C(OC)C(OC)=CC(N2N=CC3=C2C=C(C4=CC=CC5=C4C=CN5)N=C3)=C1
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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)