Tubulin polymerization-IN-92
Tubulin polymerization-IN-92, an analog of KX-01 (HY-10340), is a potent orally active tubulin polymerization inhibitor that binds tubulin with a Ka of 1.29 μM. Tubulin polymerization-IN-92 simultaneously occupies the colchicine site in β-tubulin and a cavity in α-tubulin. Tubulin polymerization-IN-92 exerts antiproliferative activity, induces G2/M cell cycle arrest and apoptosis in cancer cells. Tubulin polymerization-IN-92 inhibits tumor growth in mouse xenograft models. Tubulin polymerization-IN-92 can be used for the research of colon cancer, cervical cancer, and Paclitaxel (HY-B0015)-resistant ovarian cancer.
For research use only. We do not sell to patients.
- Formula: C31H33F2N3O3
- Molecular Weight:533.61
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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 polymerization-IN-92 (compound 8h) potently inhibits proliferation of HCT116, HeLa, A2780S, A2780T, HT29, and HUVEC cells with IC50 values of 3.5, 2.4, 15.7, 22.1, and 7.3 nM, respectively, and demonstrates activity against Paclitaxel-resistant A2780T cells[1].
Tubulin polymerization-IN-92 (5 μM; 5 min) inhibits in vitro tubulin polymerization[1].
Tubulin polymerization-IN-92 (10-30 nM; 24 h) disrupts the microtubule network in HT29, A2780S, and A2780T cells[1].
Tubulin polymerization-IN-92 (10-100 nM; 48 h) induces concentration-dependent G2/M phase arrest in HT29 cells[1].
Tubulin polymerization-IN-92 (30-100 nM; 48 h) induces late-stage apoptosis in HeLa cells[1].
Tubulin polymerization-IN-92 (10-100 nM; 14 days) inhibits colony formation in A2780S, A2780T and HT29 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT29, A2780S, A2780T
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Concentration:10; 30 nM
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Incubation Time:24 h
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Result:Induced microtubule depolymerization in HT29, A2780S, and A2780T cells.
Showed intact, organized microtubule networks in untreated cells.
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Cell Line:HT29
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Concentration:10, 30, 100 nM
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Incubation Time:48 h
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Result:Induced G2/M phase arrest in a concentration-dependent manner.
Increased the proportion of cells in G2/M phase from 8.14% (control) to 60.58% at 100 nM.
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Cell Line:HeLa
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Concentration:10, 30, 100 nM
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Incubation Time:48 h
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Result:Induced late-stage apoptosis in HeLa cells.
Exhibited 8.43% of late apoptotic cells at 30 nM.
Increased late apoptotic cells from 0.47% (control) to 25.12% at 100 nM.
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Cell Line:HT29, A2780S, A2780T
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Concentration:40, 100 nM
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Incubation Time:14 days
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Result:Significantly decreased the colony number and area of A2780S cells at 40 nM.
Completely inhibited colony formation in A2780T and HT29 cells at 100 nM.
Inhibited colony formation in A2780S
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Balb/c mice (5-6 weeks) injected with HT-29 cells[1]
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Dosage:5; 10 mg/kg
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Administration:p.o.; once daily; 10 days
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Result:Exerted favorable in vivo antitumor activity with tumor growth inhibition (TGI) rates of 58.6% and 70.1% at 5 and
10 mg/kg, respectively.
Showed no significant body weight changes at 5 mg/kg dose.
Exhibited severe toxic side
effect at 10 mg/kg.
Chemical Information
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Molecular Weight 533.61
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Formula C31H33F2N3O3
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SMILES
O=C(NCC1=CC=CC=C1)CC2=C(C=C(C=C2)C3=CC=C(C=C3)OCCN4CCN(CC4)C([C@@H]5C[C@@H]5F)=O)F
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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-92 Related Classifications
HY-183329 Related Classifications
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