2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  3. Microtubule/Tubulin Apoptosis
  4. 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.

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Tubulin-IN-57

Tubulin-IN-57 Chemical Structure

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Tubulin-IN-57 Related Antibodies

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Description

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[1].

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.

Tubulin-IN-57 Related Antibodies

Cell Proliferation Assay[1]

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 Migration Assay [1]

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.

Western Blot Analysis[1]

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 Cycle Analysis[1]

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.

Western Blot Analysis[1]

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

Tubulin-IN-57 (2 mg/kg, 4 mg/kg, intravenous administration, every 2 days for a total of 12 doses) inhibits tumor growth by suppressing both cell proliferation and shows no significant pathological changes in mice, indicating minimal toxicity at the tested doses and schedules[1].

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.
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
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Tubulin-IN-57 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tubulin-IN-57Microtubule/TubulinApoptosisTubulin InhibitorsMicrotubule-Targeting AgentsMTAsOvarian cancerInhibitorinhibitorinhibit

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