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Cevipabulin
- TTI-237
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C18H18ClF5N6O
- MW: 464.82
Description
Cevipabulin is a potent microtubule-active antitumor agent with an IC50 value of 34 nM for cytotoxicity. Cevipabulin inhibits binding of vinblastine at the Vinca alkaloid site of the αβ-tubulin heterodimer. Moreover, Cevipabulin enhances the aggregation of microtubule protein at substoichiometric concentrations and also induces aggregation of highly purified tubulin in the absence of GTP. At low concentrations with cells, Cevipabulin induces mitotic spindle perturbations that do not cause mitotic block but lead to the production of multinuclear G1 cells. Cevipabulin shows good antitumor activity in nude mouse xenograft models of human cancer.
More Information
| Parent CAS No. | 849550-05-6 |
|---|---|
| Chemical Name | (S)-5-Chloro-6-(2,6-difluoro-4-(3-(methylamino)propoxy)phenyl)-N-(1,1,1-trifluoropropan-2-yl)-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine |
| MFCD | N.A. |
| Short Description | Microtubule-active agent |
References
- N Zhang et al. Synthesis and SAR of [1,2,4]triazolo[1,5-a]pyrimidines, a class of anticancer agents with a unique mechanism of tubulin inhibition. J Med Chem. 2007 Jan 25;50(2):319-27.
- N Zhang et al. 2-cyanoaminopyrimidines as a class of antitumor agents that promote tubulin polymerization. Bioorg Med Chem Lett. 2007 Jun 1;17(11):3003-5.
- CF Beyer et al. TTI-237: a novel microtubule-active compound with in vivo antitumor activity. Cancer Res. 2008 Apr 1;68(7):2292-300.
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