1201898-17-0

溶解度:Unknown

储存条件:at -20℃ 2 years

生物活性

Vinflunine Tartrate is a tartrate salt of vinflunine that is a new microtubule inhibitor with IC50 of 18.8 nM. Vinflunine is a novel bifluorinated vinca alkaloid. At concentrations approximating the IC50 for mitotic accumulation, centromere dynamicity decreased by 44%respectively, and the time centromeres spent in a paused state increased by 63%. Vinflunine suppressed the rate of treadmilling (IC50 = 0.42 μM), but to a lesser extent than vinorelbine (IC50 = 0.10 μM) and vinblastine (IC50 = 0.066 μM). Like vinorelbine and vinblastine, vinflunine suppressed centromere dynamics at nanomolar concentrations (equivalent to those that blocked mitosis). Vinflunine, similar to vinorelbine, vinblastine and vincristine, inhibited microtubule assembly at micromolar concentrations (IC50 =3.1 μM). However, other effects, such as induction of cell cycle arrest at G2+M (associated with mitotic accumulation), disruption of the microtubular network of interphase cells and formation of paracrystals, generally required 3- to 17-fold higher concentrations of vinflunine than the other vinca alkaloids.

参考文献

[1] http://en.wikipedia.org/wiki/Vinflunine

[2] Mol Cancer Ther. 2003 May;2(5):427-36.