2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  3. Microtubule/Tubulin Apoptosis
  4. Tubulin-IN-63

Tubulin-IN-63 是一种强效的微管蛋白聚合 (tubulin polymerization) 抑制剂，靶向秋水仙碱结合位点，IC50 值为 6.03 µM。Tubulin-IN-63 可破坏微管动力学，诱导 G2/M 期阻滞和细胞凋亡 (apoptosis)，从而抑制癌细胞增殖。Tubulin-IN-63 可破坏人脐静脉内皮细胞 (HUVEC) 的毛细血管网络形成，并在 B16-F10 小鼠模型中显示出体内抗肿瘤活性。Tubulin-IN-63 可用于黑色素瘤、肺癌和肝癌等癌症的研究。

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Tubulin-IN-63

Tubulin-IN-63 Chemical Structure

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Tubulin-IN-63 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-63 is a potent tubulin polymerization inhibitor targeting the colchicine-binding site, with an IC50 of 6.03 µM. Tubulin-IN-63 disrupts microtubule dynamics, induces G2/M arrest and apoptosis, thereby suppressing cancer cell proliferation. Tubulin-IN-63 disrupts capillary network formation in human umbilical vein endothelial cells (HUVECs) and exhibits in vivo antitumor efficacy in a B16-F10 mouse model. Tubulin-IN-63 can be used for the research of cancers, such as melanoma, lung cancer, and liver cancer[1].

体外研究
(In Vitro)

Tubulin-IN-63 (compound 4a) (48 小时) 对多种癌细胞系 (B16-F10、MCF-7、Hela 和 HepG-2) 表现出强效的抗增殖活性，IC50 分别为 0.052、0.045、0.076 和 0.036 µM，同时对正常细胞系 (HUVEC、MCF-10A 和 LO2) 表现出较低的细胞毒性，IC50 分别为 751、903 和 579 nM，表明其具有选择性[1]。
Tubulin-IN-63 (48 小时) 抑制 A549 和 A2780 细胞的增殖，IC50 分别为 85.3 nM 和 42.4 nM，并且对 Paclitaxel (HY-B0015) 耐药细胞 (A549/T 和 A2780/T 细胞) 仍保持活性，IC50 分别为 172.5 nM 和 61.8 nM，表明其能够克服 Paclitaxel 相关的耐药性[1]。
Tubulin-IN-63 (10-100 nM，24 小时) 可持久抑制 HepG-2 细胞中的癌细胞生长和增殖，这表现为在无药培养 10-14 天后克隆形成存活率呈剂量依赖性降低[1]。
Tubulin-IN-63 (10-100 nM，48 小时) 在 HepG-2 细胞中以剂量依赖性方式诱导 G2/M 细胞周期阻滞和细胞凋亡[1]。
Tubulin-IN-63 (10-100 nM，0-24 小时) 以浓度依赖性方式抑制 HepG-2 细胞迁移[1]。
Tubulin-IN-63 (10-100 nM，12 小时) 在 HepG-2 细胞中引起剂量依赖性的微管网络破坏[1]。
Tubulin-IN-63 (10-100 nM，6 小时) 在 HUVECs 中破坏血管网络形成[1]。

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

Tubulin-IN-63 相关抗体:

Cell Proliferation Assay[1]

Cell Line: HepG-2
Concentration: 10, 50, 100 nM
Incubation Time: 24 h
Result: Dose-dependently restrained colony formation.
Almost completely abolished the clonogenic capacity of HepG-2 cells at 50 nM.

Cell Cycle Analysis[1]

Cell Line: HepG-2
Concentration: 10, 50, 100 nM
Incubation Time: 48 h
Result: Caused a dose-dependent G2/M phase arrest in HepG-2 cells, with the percentage of cells in G2/M increasing from 15.6% to 33.8%.

Apoptosis Analysis[1]

Cell Line: HepG-2
Concentration: 10, 50, 100 nM
Incubation Time: 48 h
Result: Caused a dose-dependent increase in apoptosis in HepG-2 cells, with total apoptotic cell percentages of 18.02%, 42.90%, and 53.73% at 10, 50, and 100 nM, respectively.

Cell Migration Assay [1]

Cell Line: HepG-2
Concentration: 10, 50, 100 nM
Incubation Time: 0, 24 h
Result: Dose-dependently inhibited the migration of HepG-2 cells, with the recovered area decreasing to 35.41% at 10 nM, 20.69% at 50 nM, and 13.91% at 100 nM.

Cell Cytotoxicity Assay[1]

Cell Line: HUVECs
Concentration: 10, 50, 100 nM
Incubation Time: 6 h
Result: Dose-dependently disrupted the formation of capillary-like networks in HUVECs.
体内研究
(In Vivo)

Tubulin-IN-63 (compound 4a) (10 mg/kg，腹腔注射，每日一次，持续 14 天) 在 B16-F10 小鼠模型中显著抑制肿瘤生长，并且与 PD-L1 抑制剂 NP19 (HY-131347) 联合使用时显示出协同作用[1]。

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

Animal Model: Male C57BL/6 mice subcutaneously injected with B16-F10 cells[1]
Dosage: 10 mg/kg
Administration: i.p., daily for 14 days
Result: Significantly suppressed tumor growth, achieving a TGI value of 69.25%.
Resulted in a pronounced synergistic antitumor effect, when combined with NP19 (5 mg/kg), with a TGI of 85.20%.
Showed no significant toxicity in vital organs (heart, liver, and kidney).
分子量

425.48

Formula

C26H23N3O3
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-63 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-63Microtubule/TubulinApoptosisDrug resistanceTubulinAntitumorColchicine binding siteQuinazoline analogsInhibitorinhibitorinhibit

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