Tubulin-IN-54
Tubulin-IN-54 is a tubulin inhibitor. Tubulin-IN-54 exhibits anti-proliferative activity against various cancer cells. Tubulin-IN-54 inhibits tubulin polymerization, disrupts microtubule networks, induces G2/M cell cycle arrest, and promotes cancer cell apoptosis. Tubulin-IN-54 demonstrates significant anti-tumor efficacy in mice bearing PC-3/TxR xenografts. Tubulin-IN-54 can be used for the study of taxane-resistant cancers (prostate cancer, melanoma).
For research use only. We do not sell to patients.
- Formula: C21H19N3O4
- Molecular Weight:377.39
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Storage:
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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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Tubulin-IN-54 (Compound 11b) (72 h) exhibits potent anti-proliferative activity against human melanoma A375 (IC50 = 0.6 nM), M14 (IC50 = 0.6 nM) and human prostate cancer PC-3 (IC50 = 1.3 nM) cells[1].
Tubulin-IN-54 (2-5 nM, 24 h) inhibits tubulin polymerization and disrupts microtubule network structures in PC-3/TxR cells[1].
Tubulin-IN-54 (0.5-5 nM, 24 h) potently inhibits colony formation and migration of PC-3/TxR cells[1].
Tubulin-IN-54 (1-5 nM, 24 h) induces G2/M cell cycle arrest and apoptosis in PC-3/TxR cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC-3/TxR cells
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Concentration:1, 2, 5 nM
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Incubation Time:24 h
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Result:Inhibited migration of PC-3/TxR cells.
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Cell Line:PC-3/TxR cells
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Concentration:1, 2, 5 nM
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Incubation Time:24 h
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Result:Induced G2/M cell cycle arrest in PC-3/TxR cells.
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Cell Line:PC-3/TxR cells
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Concentration:1, 2, 5 nM
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Incubation Time:24 h
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Result:Induced apoptosis in PC-3/TxR cells.
Downregulated the expression of anti-apoptotic protein Bcl-2.
Upregulated the expression of pro-apoptotic proteins cleaved-PARP and cleaved-caspase-3.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:PC-3/TxR cells (2.5 × 106 in 100 µL mixture of medium and Matrigel at 1:1 ratio) were subcutaneously implanted into the dorsal right flanks of 8-9-week-old male NOD scid gamma (NSG) mice[1]
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Dosage:15 mg/kg
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Administration:i.p. 5 times/week for 2 weeks
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Result:Achieved tumor growth inhibition (TGI) rates of 67% and 80% at doses of 15 mg/kg and 30 mg/kg.
Reduced the Ki67 expression.
Induced increased phosphorylation of Histone H3 (a G2/M phase arrest marker).
Increased the expression of cleaved-PARP and cleaved-caspase-3.
Reduced the expression of CD31 (a vascular marker).
Showed no acute toxicity to major organs (liver, lung, spleen, kidney).
Chemical Information
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Molecular Weight 377.39
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Formula C21H19N3O4
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SMILES
O=C(C1=CC(OC)=C(C(OC)=C1)OC)C2=NC(C3=CC=CC4=C3C=CN4)=CN2
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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-54 Related Classifications
HY-175555 Related Classifications
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