Tubulin-IN-57
Tubulin-IN-57 is a Tubulin inhibitor. Tubulin-IN-57 is a potent antiproliferative agent that inhibits clonogenic formation, migration, and invasion of ovarian cancer cells. Tubulin-IN-57 inhibits tubulin polymerization, which in turn induces G2/M arrest and apoptosis in SKOV3 cells. Tubulin-IN-57 demonstrates potent antitumor activity without observable toxicity in an SKOV3 xenograft model. Y60S can be used for the study of ovarian cancer.
For research use only. We do not sell to patients.
- Formula: C26H24N4O3
- Molecular Weight:440.49
-
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]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
In Vitro
Tubulin-IN-57 (Compound Y60s) (72 h) exhibits potent antiproliferative activity (SKOV3 IC50 = 0.025 μM; A549 IC50 = 0.026 μM)[1].
Tubulin-IN-57 (25-200 nM, 6 days) inhibits the colony formation and proliferation of SKOV3 and A549 cells[1].
Tubulin-IN-57 (25-200 nM, 0-24 h) inhibits the migration of SKOV3 and A549 cells[1].
Tubulin-IN-57 (25-200 nM, 48 h) induces cell apoptosis and alters the expression of apoptosis-related proteins of SKOV3 and A549[1].
Tubulin-IN-57 (25,50,100,200 nM, 24 h) induces the G2/M phase cell cycle arrest in SKOV3 and A549 cells[1].
Tubulin-IN-57 (10-40 μM) inhibits polymerization and demonstrates dose-dependent inhibition of tubulin polymerization, with complete inhibition observed at 20 μM[1].
Tubulin-IN-57 (20 nM) causes severe microtubule disruption and disorganization in SKOV3[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:SKOV3, A549 cells
-
Concentration:25 nM, 50 nM, 100 nM, 200 nM
-
Incubation Time:6 days
-
Result:Dose-dependently inhibited colony formation in SKOV3 cells.
Revealed significant inhibition in SKOV3 cells starting at 25 nM.
-
Cell Line:SKOV3, A549 cells
-
Concentration:25 nM, 50 nM, 100 nM, 200 nM
-
Incubation Time:0 h, 6 h, 12 h, 24 h
-
Result:Dose-dependently inhibited SKOV3 cell migration.
A similar dose-dependent inhibition was observed in A549 cells.
Resulted in a dose-dependent reduction in wound closure in both SKOV3 and A549 cells over 24 h.
-
Cell Line:SKOV3, A549 cells
-
Concentration:100 nM
-
Incubation Time:48 h
-
Result:Dose-dependently downregulated Bcl-2 and upregulated cleaved PARP, cleaved caspase-3, and cleaved caspase-9 in both SKOV3 and A549 cells.
-
Cell Line:SKOV3, A549 cells
-
Concentration:25 nM, 50 nM, 100 nM, 200 nM
-
Incubation Time:24 h
-
Result:Resulted in G2/M phase arrest in both SKOV3 and A549 cells.
-
Cell Line:SKOV3, A549 cells
-
Concentration:25 nM, 50 nM, 100 nM, 200 nM
-
Incubation Time:24 h
-
Result:Dose-dependently increased cyclin B1 expression and decreased Cdc25c expression in both cell lines.
Cdc2 expression showed cell line-specific differences: in SKOV3 cells, the reduction was not apparent across the treatment range, whereas in A549 cells, Cdc2 levels remained largely unchanged at 50 nM but began to decrease at 100 nM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Female BALB/c nude mice (6-8 weeks old) received a subcutaneous injection of 1 × 10⁸ SKOV3 cells into the right flank[1].
-
Dosage:2 mg/kg, 4 mg/kg
-
Administration:Intravenous administration, every 2 days for a total of 12 doses
-
Result:Significantly inhibited tumor growth compared to the control, with TGI values of 35.4%, 44.3%, respectively.
Suggested a favorable safety profile for these doses and schedules.
Significantly decreased Ki-67 expression, a marker of cell proliferation.
Chemical Information
-
Molecular Weight 440.49
-
Formula C26H24N4O3
-
SMILES
CCOC1=CC=C(C=C1)C2=C3C(C(N([C@@H]3C4=CC=CC=C4OC)CC5=CC=NC=C5)=O)=NN2
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
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-57 Related Classifications
HY-178325 Related Classifications
Powered by Bioz