Tubulin inhibitor 24

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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 inhibitor 24 

Tubulin inhibitor 24 是一种有效的 tubulin 抑制剂。Tubulin inhibitor 24 抑制微管蛋白聚合。Tubulin inhibitor 24 以浓度依赖性方式诱导细胞周期停滞在 G2/M 期。Tubulin inhibitor 24 具有抗肿瘤活性且无明显毒性。

Tubulin inhibitor 24

Tubulin inhibitor 24 Chemical Structure

CAS No. : 2415761-65-6

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生物活性

Tubulin inhibitor 24 is a potent tubulin inhibitor. Tubulin inhibitor 24 inhibits tubulin polymerization. Tubulin inhibitor 24 induces cell cycle arrest at the G2/M phase in a concentration-dependent manner. Tubulin inhibitor 24 shows antitumor activity with no obvious toxicity[1].

体外研究
(In Vitro)

Tubulin inhibitor 24 (compound 1b) () shows high antiproliferative activity with IC50s of 0.021, 0.047, 0.003, 0.048 µM for Hela, MCF-7, A549, HCT-116, B16-F10 cells, respectively[1].
Tubulin inhibitor 24 inhibites tubulin polymerization with an IC50 value of 2.1 µM[1].
Tubulin inhibitor 24 (5, 10 nM) induces cell cycle arrest at the G2/M phase in a concentration-dependent manner[1].
Tubulin inhibitor 24 (10, 20, 40 nM; 24 h) inhibits MCF-7 cancer cells migration in a dose-dependent manner[1].
Tubulin inhibitor 24 (40 nM; 6 h) destabilizes microtubule by inhibiting tubulin polymerization and disturbing microtubule networks in B16-F10 cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: Hela, MCF-7, A549, HCT-116, B16-F10 cells
Concentration: 0.00098, 0.0039, 0.016, 0.0625, 0.25, 1.0, 4.0, 16, 64 µM
Incubation Time: 48 h
Result: Showed high antiproliferative activity with IC50s of 0.021, 0.047, 0.003, 0.048 µM for Hela, MCF-7, A549, HCT-116, B16-F10 cells, respectively.

Cell Cycle Analysis[1]

Cell Line: MCF-7 cells
Concentration: 5, 10 nM
Incubation Time: 48 h
Result: Cells were arrested at the G2/M phase in a concentration-dependent manner.

体内研究
(In Vivo)

Tubulin inhibitor 24 (10, 20 mg/kg; i.p.; per day for 16 days) shows antitumor activity with no obvious toxicity[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 4-6 weeks, male C57/BL mice (B16e-10 tumor model)[1]
Dosage: 10, 20 mg/kg (formulated in 5% DMSO, 40% PEG-300 and 55% saline)
Administration: I.p.; per day, 16 days
Result: Showed antitumor activity with no obvious toxicity.

分子量

375.42

Formula

C22H21N3O3
CAS 号

2415761-65-6
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]. Li G,et al. Design, synthesis, and bioevaluation of pyrazolo[1,5-a]pyrimidine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site with potent anticancer activities. Eur J Med Chem. 2020; 202:112519.

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