Tubulin polymerization-IN-89
Tubulin polymerization-IN-89 is a tubulin polymerization inhibitor. Tubulin polymerization-IN-89 binds to the colchicine-binding site on tubulin heterodimers, disrupting tubulin polymerization and microtubule formation. Tubulin polymerization-IN-89 induces apoptosis in melanoma cells and arrests the cell cycle at the G2/M phase. Tubulin polymerization-IN-89 can be used in studies related to metastatic melanoma.
For research use only. We do not sell to patients.
- Formula: C18H17N5O2
- Molecular Weight:335.36
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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
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Biological Activity
Tubulin polymerization-IN-89 (compound 9d) (100 nM; 24 h) disrupts the microtubule network, induces G2/M phase cell cycle arrest, and triggers apoptosis in A375 cells by activating cleaved caspase-3 and cleaved PARP[1].
Tubulin polymerization-IN-89 exhibits potent cytotoxicity in various melanoma cell lines, with the following GI50 values: A375 (15.4 nM), RPMI-7951 (17.0 nM), A2058 (13.8 nM), and the paclitaxel-resistant strain A375/TxR (24.7 nM)[1].
Tubulin polymerization-IN-89 (20-40 nM; 24 h) inhibits migration and invasion of A375/TxR cells[1].
Tubulin polymerization-IN-89 (25-100 nM) completely abolishes colony formation in A375 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A375 melanoma cells
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Concentration:100 nM
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Incubation Time:24 h
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Result:Induced G2/M cell cycle arrest, with 80% of cells in G2/M phase.
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Cell Line:paclitaxel-resistant A375/TxR cells
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Concentration:20, 40 nM
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Incubation Time:24 h
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Result:Inhibited cell migration by 86% at 40 nM.
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUClast | AUCinf | MRT0-inf |
|---|---|---|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | i.p. | 1.49 h | 8.34 min | 316 ng/mL | 263 ng·h/mL | 271 ng·h/mL | 1.37 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD scid gamma (NSG) (female, 6−8 weeks old)[1]
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Dosage:10 mg/kg; 15 mg/kg
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Administration:i.p.; 3x per week
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Result:Reduced mean ex vivo tumor volume and tumor weight.
Decreased Ki67-positive area.
Increased cleaved caspase-3-positive area.
Increased CD45-positive area.
Reduced viable tumor area.
Chemical Information
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Molecular Weight 335.36
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Formula C18H17N5O2
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SMILES
CCNC1=NC2=CC=CC=C2N3C1=NN=C3C4=CC(O)=C(OC)C=C4
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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 polymerization-IN-89 Related Classifications
HY-182039 Related Classifications
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