Tubulin polymerization-IN-9

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Tubulin polymerization-IN-9 

Tubulin polymerization-IN-9 是一种有效的微管蛋白 (tubulin) 抑制剂，IC50 为 1.82 μM。Tubulin polymerization-IN-9 能引起细胞周期阻滞在 G2/M 期，诱导 K562 细胞凋亡 (apoptosis) 和线粒体去极化。Tubulin polymerization-IN-9 具有强效的抗血管和抗肿瘤活性。

Tubulin polymerization-IN-9

Tubulin polymerization-IN-9 Chemical Structure

CAS No. : 2485020-93-5

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生物活性

Tubulin polymerization-IN-9 is a potent tubulin inhibitor with IC50 of 1.82 μM. Tubulin polymerization-IN-9 causes cell cycle arrest at G2/M phase, and induces cell apoptosis and depolarized mitochondria of K562 cells. Tubulin polymerization-IN-9 has potent anti-vascular and antitumor activities[1].

IC50 & Target

IC50: 1.82 μM (tubulin)[1]
体外研究
(In Vitro)

Tubulin polymerization-IN-9 (compound 11k) (0.1, 1, 10 μM; 72 hours) has potent activity against these three cancer cell lines with IC50 values ranging from 0.287 to 0.621 μM[1].
Tubulin polymerization-IN-9 (0.15, 0.3 and 0.6 μM; 24 hours) induces a dose-dependent collapse of the microtubule networks[1].
Tubulin polymerization-IN-9 (0.15, 0.3 and 0.6 μM; 48 hours) observes a gradual accumulation of cells at G2/M phase in K562 cells[1].
Tubulin polymerization-IN-9 (0.15, 0.3 and 0.6 μM; 72 hours) effectively induces cell apoptosis in K562 cells in a concentration-dependent manner[1].
Tubulin polymerization-IN-9 (0.15, 0.3 and 0.6 μM; 24 hours) causes mitochondrial depolarization of K562 cells in the process of apoptosis[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: K562 HepG2 and HCT-8 cells[1]
Concentration: 0.1, 1, 10 μM
Incubation Time: 72 hours
Result: Showed potent activity against these three cancer cell lines with IC50 values ranging from 0.287 to 0.621 μM.

Immunofluorescence

Cell Line: K562 cells[1]
Concentration: 0.15, 0.3 and 0.6 μM
Incubation Time: 24 hours
Result: Induced a dose-dependent collapse of the microtubule networks.

Cell Cycle Analysis

Cell Line: K562 cells[1]
Concentration: 0.15, 0.3 and 0.6 μM
Incubation Time: 48 hours
Result: Observed a gradual accumulation of cells at G2/M phase in K562 cells.

Apoptosis Analysis

Cell Line: K562 cells[1]
Concentration: 0.15, 0.3 and 0.6 μM
Incubation Time: 72 hours
Result: Effectively induced cell apoptosis in K562 cells in a concentration-dependent manner.

体内研究
(In Vivo)

Tubulin polymerization-IN-9 (15 and 30 mg/kg; IV; once a day, for 21 days) effectively suppresses the tumor volume and reduces tumor weight by 71.1% at a dose of 30 mg/kg[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male ICR mice (5 weeks; injected with H22 cells; n=6)[1]
Dosage: 15 and 30 mg/kg
Administration: IV; once a day, for 21 days
Result: Effectively suppressed the tumor volume and reduced tumor weight by 71.1% at a dose of 30 mg/kg.

分子量

420.32

Formula

C19H19NO5Se
CAS 号

2485020-93-5
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.
参考文献

  • [1]. Zhu H, Sun H, Liu Y, et al. Design, synthesis and biological evaluation of vinyl selenone derivatives as novel microtubule polymerization inhibitors. Eur J Med Chem. 2020;207:112716.

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