2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  3. Microtubule/Tubulin Apoptosis
  4. Tubulin-IN-54

Tubulin-IN-54 是一种微管蛋白 (tubulin) 抑制剂。Tubulin-IN-54 对多种癌细胞表现出抗增殖活性。Tubulin-IN-54 抑制微管蛋白聚合作用，破坏微管网络，诱导 G2/M 期细胞周期阻滞，并促进癌细胞凋亡 (apoptosis)。Tubulin-IN-54 在 PC-3/TxR 异种移植瘤的小鼠中展示出显著的抗肿瘤效能。Tubulin-IN-54 可用于研究紫杉烷耐药性癌症 (前列腺癌、黑色素瘤)。

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Tubulin-IN-54

Tubulin-IN-54 Chemical Structure

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Tubulin-IN-54 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-54 is a tubulin inhibitor. Tubulin-IN-54 exhibits anti-proliferative activity against various cancer cells. Tubulin-IN-54 inhibits tubulin polymerization, disrupts microtubule networks, induces G2/M cell cycle arrest, and promotes cancer cell apoptosis. Tubulin-IN-54 demonstrates significant anti-tumor efficacy in mice bearing PC-3/TxR xenografts. Tubulin-IN-54 can be used for the study of taxane-resistant cancers (prostate cancer, melanoma)[1].

体外研究
(In Vitro)

Tubulin-IN-54 (Compound 11b) (72 h) 对人黑色素瘤细胞 A375 (IC50 = 0.6 nM)、M14 (IC50 = 0.6 nM) 和人前列腺癌细胞 PC-3 (IC50 = 1.3 nM) 表现出强效的抗增殖活性[1]。
Tubulin-IN-54 (2-5 nM, 24 h) 在 PC-3/TxR 细胞中抑制微管蛋白聚合作用并破坏微管网络结构[1]。
Tubulin-IN-54 (0.5-5 nM, 24 h) 强效抑制 PC-3/TxR 细胞的集落形成和迁移[1]。
Tubulin-IN-54 (1-5 nM, 24 h) 在 PC-3/TxR 细胞中诱导 G2/M 期细胞周期阻滞和细胞凋亡[1]。

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

Tubulin-IN-54 相关抗体:

Cell Migration Assay [1]

Cell Line: PC-3/TxR cells
Concentration: 1, 2, 5 nM
Incubation Time: 24 h
Result: Inhibited migration of PC-3/TxR cells.

Cell Cycle Analysis[1]

Cell Line: PC-3/TxR cells
Concentration: 1, 2, 5 nM
Incubation Time: 24 h
Result: Induced G2/M cell cycle arrest in PC-3/TxR cells.

Apoptosis Analysis[1]

Cell Line: PC-3/TxR cells
Concentration: 1, 2, 5 nM
Incubation Time: 24 h
Result: Induced apoptosis in PC-3/TxR cells.
Downregulated the expression of anti-apoptotic protein Bcl-2.
Upregulated the expression of pro-apoptotic proteins cleaved-PARP and cleaved-caspase-3.
体内研究
(In Vivo)

Tubulin-IN-54 (Compound 11b) (15 mg/kg，腹腔注射，每周 5 次，持续 2 周) 在 PC-3/TxR 前列腺癌异种移植瘤的 NSG 雄性小鼠中展示出显著的抗肿瘤效能[1]。

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

Animal Model: PC-3/TxR cells (2.5 × 106 in 100 µL mixture of medium and Matrigel at 1:1 ratio) were subcutaneously implanted into the dorsal right flanks of 8-9-week-old male NOD scid gamma (NSG) mice[1]
Dosage: 15 mg/kg
Administration: i.p. 5 times/week for 2 weeks
Result: Achieved tumor growth inhibition (TGI) rates of 67% and 80% at doses of 15 mg/kg and 30 mg/kg.
Reduced the Ki67 expression.
Induced increased phosphorylation of Histone H3 (a G2/M phase arrest marker).
Increased the expression of cleaved-PARP and cleaved-caspase-3.
Reduced the expression of CD31 (a vascular marker).
Showed no acute toxicity to major organs (liver, lung, spleen, kidney).
分子量

377.39

Formula

C21H19N3O4
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-54 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-54Microtubule/TubulinApoptosisPC-3/TxRtubulinprostate cancermelanomaapoptosisInhibitorinhibitorinhibit

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