1. Cell Cycle/DNA Damage Cytoskeleton
  2. Microtubule/Tubulin
  3. Tubulin-IN-52

Tubulin-IN-52 是一种 tubulin 抑制剂。Tubulin-IN-52 对包括前列腺癌、肺癌和卵巢癌在内的多种癌细胞类型均表现出显著的细胞毒性 (IC50 = 0.9-3.8 μM)。Tubulin-IN-52 能显著抑制肿瘤的生长且无明显毒性。Tubulin-IN-52 可用于癌症相关研究。

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Tubulin-IN-52

Tubulin-IN-52 Chemical Structure

CAS No. : 2099064-75-0

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Tubulin-IN-52 is a tubulin inhibitor. Tubulin-IN-52 demonstrates significant cytotoxicity toward a variety of cancer cell types including prostate, lung, and ovarian cancers with strong activity toward highly aggressive cancer lines (IC50 = 0.9-3.8 mM). Tubulin-IN-52 significantly inhibits the growth of established tumors without noticeable toxicity. Tubulin-IN-52 can be used for the study of cancer[1].

体外研究
(In Vitro)

Tubulin-IN-52 (Compound 18) (1-10 μM, 72 h) 在 A549 细胞系及前列腺癌细胞系 PC3 和 PC3MLN4 中可诱导显著细胞毒性[1]
Tubulin-IN-52 (0.0032-50 μM) 对多种癌细胞表现出高度细胞毒性,其 EC50 值分别为:2.4 μM (H157)、1.6 μM (Calu1)、1.4 μM (A549)、1.6 μM (PC3)、0.9 μM (PC3MLN4) 和1.0 μM (SKOV3)[1]
Tubulin-IN-52 (1 μM, 24 h) 可诱导 PC3MLN4 细胞发生 G2/M 期周期阻滞[1]
Tubulin-IN-52 (1 μM, 48 h) 会破坏 PC3MLN4 细胞的微管动力学[1]

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

Cell Viability Assay[1]

Cell Line: PC3MLN4, PC3 and A549 cells
Concentration: 1, 10 μM
Incubation Time: 72 h
Result: Induced significant cytotoxicity at 1 and 10 μM.

Cell Cycle Analysis[1]

Cell Line: PC3MLN4 cells
Concentration: 1 μM
Incubation Time: 24 h
Result: Induced G2M cell cycle arrest in PC3MLN4 cells.

Western Blot Analysis[1]

Cell Line: PC3MLN4, PC3 and A549 cells
Concentration: 1 μM
Incubation Time: 48 h
Result: Increased the level of cyclin B1.
体内研究
(In Vivo)

Tubulin-IN-52 (Compound 18) (30 mg/kg, 腹腔注射, 每周三次, 持续两周) 在 PC3MLN4 异种移植小鼠模型中显示出对肿瘤生长的显著抑制作用[1]

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

Animal Model: PC3MLN4 cells (106)-derived subcutaneous xenograft athymic male mice (eight weeks)[1]
Dosage: 30 mg/kg
Administration: i.p. 3 times a week for two weeks
Result: Showed tumor volume (day 15) of 43.2 mm3 while that of the control group (C) is 118.8 mm3.
Showed treatment-to-control (T/C) ratio at the last time point of 0.36, below the T/C 0.45 threshold that defines active antitumor activity.
Showed no noticeable toxicity.
分子量

380.40

Formula

C20H20N4O4

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
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  • 稀释计算器

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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.

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产品名称:
Tubulin-IN-52
目录号:
HY-177138
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