Tubulin-IN-62
Tubulin-IN-62 is a tubulin inhibitor targeting the colchicine-binding site. Tubulin-IN-62 exhibits IC50 values of 17.2 nM and 19.3 nM against SKOV3 and HCC827 cells, respectively. Tubulin-IN-62 inhibits microtubule polymerization, arrests the cell cycle at the G2/M phase, and induces apoptosis. Tubulin-IN-62 demonstrates significant antitumor efficacy in vivo with good tolerability. Tubulin-IN-62 can be used in ovarian cancer and non-small cell lung cancer (NSCLC) research.
For research use only. We do not sell to patients.
- Formula: C21H23N5O3
- Molecular Weight:393.44
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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-62 (compound (S)-Q31) (10-80 nM, 10 days) inhibits colony-formation ability of SKOV3 and HCC827 cells[1].
Tubulin-IN-62 (10-80 nM, 24 h) suppresses the migration of SKOV3 and HCC827 cells[1].
Tubulin-IN-62 (10-80 nM, 48 h) exerts antiproliferative effect and induces apoptosis in SKOV3 and HCC827 cells[1].
Tubulin-IN-62 (5-40 nM, 48 h) induces apoptosis in SKOV3 and HCC827 cells[1].
Tubulin-IN-62 (10-80 nM, 24 h) arrests SKOV3 and HCC827 cells at the G2/M phase[1].
Tubulin-IN-62 (10-80 nM, 48 h) induces G2/M phase cell cycle arrest by downregulating the expression of Cdc-25c, cyclin B1, and Cdc-2 in SKOV3 and HCC827 cells [1].
Tubulin-IN-62 (2.5-20 μM, 80 min) exhibits inhibitory activity on tubulin polymerization in SKOV3 and HCC827 cells[1].
Tubulin-IN-62 (40 nM, 24 h) inhibits microtubule polymerization and disrupts microtubule networks in SKOV3 and HCC827 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SKOV3 and HCC827 cell lines
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Concentration:10, 20, 40, 80 nM
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Incubation Time:10 Days
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Result:Reduced both the colony number and area in both SKOV3 and HCC827 cells in a dose-dependent manner, with complete inhibition of clonogenic potential observed at 40 nM.
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Cell Line:SKOV3 and HCC827 cell lines
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Concentration:0, 10, 20, 40, and 80 nM
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Incubation Time:24 h
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Result:Inhibited the migration of SKOV3 cells in a dose-dependent manner after 24 h.
Reduced the number of migrated cells from 4110 (untreated control) to 2433, representing 59.0 % of the control level in SKOV3 cells.
Reduced the number of migrated cells from 332 (untreated control) to 60 at 80 nM in HCC827 cells.
Inhibited the wound closure rate from 52.8% to 7.5 % in SKOV3 cells.
Decreased the closure rate from 70.4 % to 13.1 % in HCC827 cells.
Induced significant cytotoxicity alongside the observed inhibition at this highest concentration.
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Cell Line:SKOV3 and HCC827 cell lines
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Concentration:10, 20, 40, 80 nM
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Incubation Time:48 h
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Result:Resulted in dose-dependent increases in the total apoptosis rates in SKOV3 cells, reaching 11.29 %, 24.80 %, 32.65 %, and 35.11 % at 10, 20, 40, and 80 nM, respectively.
Increased the apoptosis rates from 2.80 % (control) to 3.23 %, 6.10 %, 6.56 %, and 16.01 % at t10, 20, 40, and 80 nM, respectively in HCC827 cells.
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Cell Line:SKOV3 and HCC827 cell lines
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Concentration:5, 10, 20, 40nM
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Incubation Time:48 h
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Result:Reduced the expression of the anti-apoptotic protein Bcl-2 and dose dependently upregulated the levels of pro-apoptotic proteins Cleaved PARP, Cleaved Caspase-9, Cleaved Caspase-3, and Bax in both SKOV3 and HCC827 cells.
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Cell Line:SKOV3 and HCC827 cell lines
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Concentration:10, 20, 40, 80 nM
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Incubation Time:24 h
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Result:Induced dose-dependent G2/M phase arrest in SKOV3 cells, with the proportion of arrested cells rising to 25.96%, 42.01%, 76.32%, and 72.54% at 10, 20, 40, and 80 nM, respectively.
Induced G2/M phase arrest in HCC827 cells,with 30.82 %, 54.01 %, 87.16 %, and 88.24 % at 10, 20, 40, and 80 nM, respectively
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Cell Line:SKOV3 and HCC827 cell lines
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Concentration:10, 20, 40, 80 nM
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Incubation Time:48 h
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Result:Reduced the expression levels of cyclin B1, Cdc-2, and Cdc-25c.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SKOV3 cells (5 × 106 SKOV3 cells, s.c.)-induced female Balb/c mice[1]
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Dosage:2 mg/kg or 4 mg/kg
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Administration:i.v., every other day (q2d) for a total of 12 doses
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Result:Demonstrated significant tumor growth inhibition (TGI), with reductions of 63.79 %, 74.12 %, and 62.94 %, respectively.
Remained body weights stable across all group.
Reduced the expression of the proliferation marker Ki-67 to a greater extent than paclitaxel, particularly at the 4 mg/ kg dose.
Decreased the expression of the anti-apoptotic protein Bcl-2 and increased the expression of the apoptosis marker cleaved PARP in a dose-dependent manner.
Chemical Information
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Molecular Weight 393.44
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Formula C21H23N5O3
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SMILES
CC1=CC(C(N2)=C[C@@H](C3=CC(OC)=C(OC)C(OC)=C3)N4C2=NN=N4)=CC(C)=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)
Tubulin-IN-62 Related Classifications
HY-179385 Related Classifications
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