917111-44-5

N-乙基-N'-[2-甲氧基-4-[5-甲基-4-[[(1S)-1-(3-吡啶基)丁基]氨基]-2-嘧啶基]苯基]脲

917111-44-5

编号ABP000307 化学名称N-乙基-N'-[2-甲氧基-4-[5-甲基-4-[[(1S)-1-(3-吡啶基)丁基]氨基]-2-嘧啶基]苯基]脲 英文名称 CYT997/ MDL: MFCD18206787 分子式C24H30N6O2 分子量434.541 纯度 >99%

化学名称 : N-乙基-N'-[2-甲氧基-4-[5-甲基-4-[[(1S)-1-(3-吡啶基)丁基]氨基]-2-嘧啶基]苯基]脲

CAS : 917111-44-5

英文名称: CYT997/

英文同义词: CYT997

溶解度:Unknown

储存条件:at -20℃ 2 years

生物活性

CYT997, a synthetic small molecule optimized for antiproliferative activity in a panel of cell-based assays, in which the compound shows an IC50 of between 1 and 100 nmol/L across a panel of cancer cell lines. The compound inhibits the polymerization of tubulin with an IC50 of ~3 μmol/L.CYT997 causes a significant increase of cells in the G2-M phase of the cell cycle.Caspase-3 activation is also observed in cells treated with CYT997 along with the generation of poly(ADP-ribose) polymerase.CYT997 exhibits vascular disrupting activity as measured in vitro by effects on the permeability of human umbilical vein endothelial cell monolayers, and in vivo by effects on tumor blood flow. CYT997 possesses a useful combination of pharmacologic and pharmacokinetic properties and has considerable potential as a novel anticancer agent.

参考文献

[1] Burns, C. J., E. Fantino, et al. (2009).Mol Cancer Ther 8(11): 3036-3045.

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