2. Cell Cycle/DNA Damage Cytoskeleton Membrane Transporter/Ion Channel Apoptosis
  3. Microtubule/Tubulin P-glycoprotein Apoptosis CDK Bcl-2 Family
  4. Tubulin-IN-66

Tubulin-IN-66 是一种微管蛋白 (tubulin) 与 P-gp 抑制剂，对癌细胞具有抗增殖活性。Tubulin-IN-66 可与微管蛋白 β 亚基 Cys239 位的 Colchicine (HY-16569) 结合位点共价结合，抑制微管蛋白聚合并破坏微管网络。Tubulin-IN-66 可抑制 P-gp 功能以克服多药耐药性。Tubulin-IN-66 可将细胞周期阻滞于 G2/M 期，并诱导细胞凋亡 (apoptosis)。Tubulin-IN-66 可抑制癌细胞的集落形成与迁移。Tubulin-IN-66 可用于乳腺癌等肿瘤的研究。

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Tubulin-IN-66

Tubulin-IN-66 Chemical Structure

CAS No. : 3110538-32-1

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Tubulin-IN-66 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Tubulin-IN-66 is a tubulin (tubulin) and P-gp inhibitor with antiproliferative activity against cancer cells. Tubulin-IN-66 covalently binds to the Colchicine (HY-16569)-binding site at Cys239 of the β-tubulin subunit, inhibits tubulin polymerization and disrupts the microtubule network. Tubulin-IN-66 inhibits P-gp function to overcome multidrug resistance. Tubulin-IN-66 arrests the cell cycle at the G2/M phase and induces apoptosis (apoptosis). Tubulin-IN-66 inhibits colony formation and migration of cancer cells. Tubulin-IN-66 can be used in the research of tumors such as breast cancer[1].

体外研究
(In Vitro)

Tubulin-IN-66 (compound 10v) (48 h) 可强效抑制 HT-1080、MCF-7 和 MDA-MB-231 癌细胞的增殖，IC50 值分别为 0.30 μM、0.24 μM 和 0.48 μM[1]。
Tubulin-IN-66 (50-200 nM; 8 days) 可以浓度依赖的方式强效抑制 HT-1080 和 MCF-7 细胞的集落形成[1]。
Tubulin-IN-66 (150-350 nM; 12-4 h) 可以浓度依赖的方式有效抑制 HT-1080 细胞的迁移能力[1]。
Tubulin-IN-66 (5-30 μM; 90 min) 可以浓度依赖的方式抑制纯化微管蛋白的聚合[1]。
Tubulin-IN-66 (150-450 nM; 24 h) 可呈浓度依赖性将 HT-1080 细胞阻滞于细胞周期的 G2/M 期，同时伴随 Cyclin B1、CDK1 和 p-H3 的表达上调[1]。
Tubulin-IN-66 (150-450 nM; 48 h) 可以浓度依赖的方式诱导 HT-1080 细胞发生早期凋亡 ，其机制涉及 Bax 表达上调和 Bcl-2 表达下调[1]。
Tubulin-IN-66 (150-450 nM; 48 h) 可呈浓度依赖性降低 HT-1080 细胞的线粒体膜电位[1]。
Tubulin-IN-66 (48 h) 可强效抑制阿霉素耐药 MCF-7/ADM 细胞的增殖，处理 48 h 后的 IC50 为 0.30 μM，其耐药指数为 1.25，显示出极低的耐药性[1]。
Tubulin-IN-66 (5-10 μM; 15 min) 可抑制 MCF-7/ADM 细胞中 P-gp 的功能[1]。
Tubulin-IN-66 (48 h) 对人正常细胞 HUVEC 和 293T 表现出细胞毒性，IC50 值分别为 0.64 μM 和 0.34 μM[1]。

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

Tubulin-IN-66 相关抗体:

Cell Proliferation Assay[1]

Cell Line: HT-1080 fibrosarcoma cells, MCF-7 breast cancer cells
Concentration: 50, 100, 200 nM
Incubation Time: 8 days
Result: Inhibited colony formation in both cell lines in a concentration-dependent manner, with near-complete inhibition observed at the highest tested concentration.

Cell Cycle Analysis[1]

Cell Line: HT-1080 fibrosarcoma cells
Concentration: 150, 300, 450 nM
Incubation Time: 24 h
Result: Induced concentration-dependent G2/M phase cell cycle arrest, with a corresponding reduction in G0/G1 phase cell proportion.
Upregulated Cyclin B1, CDK1, and p-H3 protein expression in a concentration-dependent manner via Western blot.
体内研究
(In Vivo)

Tubulin-IN-66 (10-50 mg/kg；腹腔注射；每 2 天 1 次；共 14 天) 在小鼠 4T1 乳腺癌模型中展现出剂量依赖性的体内抗肿瘤功效[1]。

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

Animal Model: BALB/c mice treated 4T1 cells (female, 6-8 weeks of age)[1]
Dosage: 10 mg/kg; 20 mg/kg; 50 mg/kg
Administration: i.p.; every other day; 14 days
Result: Showed no significant intergroup differences in mouse body weight, with no observable adverse effects.
Significantly decreased tumor volume and weight in a dose-dependent manner, with tumor growth inhibition (TGI) values of 46.76% (10 mg/kg), 53.96% (20 mg/kg), and 64.51% (50 mg/kg).
Exhibited no obvious pathological injury in major organs (heart, liver, spleen, lung, kidney) via hematoxylin and eosin (H&E) staining.
分子量

412.44

Formula

C22H24N2O6
CAS 号
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-66 相关分类

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  • 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-663110538-32-1Microtubule/TubulinP-glycoproteinApoptosisCDKBcl-2 FamilyP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Cyclin dependent kinasetubulin polymerizationHT-1080colchicine binding siteβ-Cys239breast cancerMDA-MB-231fibrosarcomamicrotubule networksMCF-7Inhibitorinhibitorinhibit

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