2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  3. Microtubule/Tubulin Apoptosis
  4. Tubulin-IN-57

Tubulin-IN-57 是一种 Tubulin 抑制剂。Tubulin-IN-57 是一种强效抗增殖剂，可抑制卵巢癌细胞的克隆形成、迁移和侵袭。Tubulin-IN-57 抑制微管蛋白聚合，进而诱导 SKOV3 细胞发生G2/M期阻滞和凋亡 (apoptosis)。在 SKOV3 异种移植瘤模型中，Tubulin-IN-57表现出显著的抗肿瘤活性，且未观察到明显的毒性。Tubulin-IN-57 可用于卵巢癌的研究。

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Tubulin-IN-57

Tubulin-IN-57 Chemical Structure

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Tubulin-IN-57 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

Tubulin-IN-57 (Compound Y60s) 表现出强效抗增殖活性 (SKOV3 IC50 = 0.025 μM；A549 IC50 = 0.026 μM)[1]。
Tubulin-IN-57 (25-200 nM，6 天) 抑制 SKOV3 和 A549 细胞的克隆形成和增殖[1]。
Tubulin-IN-57 (25-200 nM，0-24 小时) 抑制 SKOV3 和 A549 细胞的迁移[1]。
Tubulin-IN-57 (25-200 nM，48 小时) 诱导 SKOV3 和 A549 细胞凋亡并改变了凋亡相关蛋白的表达[1]。
Tubulin-IN-57 (25、50、100、200 nM，24 小时) 可诱导 SKOV3 和 A549 细胞发生 G2/M 期细胞周期阻滞[1]。
Tubulin-IN-57 (10-40 μM) 能抑制微管蛋白聚合，并表现出剂量依赖性的抑制作用，在 20 μM 时可完全抑制微管蛋白聚合[1]。
Tubulin-IN-57 (20 nM) 可导致 SKOV3 细胞中微管严重破坏和紊乱[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Tubulin-IN-57 相关抗体:

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.
体内研究
(In Vivo)

Tubulin-IN-57 (2 mg/kg、4 mg/kg，静脉注射，每 2 天一次，共 12 次) 通过抑制细胞增殖来抑制肿瘤生长，并且在小鼠中未显示明显的病理变化，表明在测试剂量和方案下毒性最小[1]。

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.
分子量

440.49

Formula

C26H24N4O3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Tubulin-IN-57 相关分类

  • 摩尔计算器

  • 稀释计算器

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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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