Tubulin inhibitor 24

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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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