(-)-N-[4-(2,2-二甲基丙酰基)-5-[[2-(乙基氨基)乙磺酰胺]甲基]-5-苯基-4,5-二氢-1,3,4

中文名称:

(-)-N-[4-(2,2-二甲基丙酰基)-5-[[2-(乙基氨基)乙磺酰胺]甲基]-5-苯基-4,5-二氢-1,3,4-噻二唑-2-基]-2,2-二甲基丙酰胺

中文同义词:

(-)-N-[4-(2,2-二甲基丙酰基)-5-[[2-(乙基氨基)乙磺酰胺]甲基]-5-苯基-4,5-二氢-1,3,4-噻二唑-2-基]-2,2-二甲基丙酰胺;EG5变构抑制剂(LITRONESIB)

英文名称:

(-)-N-[4-(2,2-Dimethylpropanoyl)-5-[[2-(ethylamino)ethanesulfonamido]methyl]-5-phenyl-4,5-dihydro-1,3,4-thiadiazol-2-yl]-2,2-dimethylpropanamide

英文同义词:

(-)-N-[4-(2,2-Dimethylpropanoyl)-5-[[2-(ethylamino)ethanesulfonamido]methyl]-5-phenyl-4,5-dihydro-1,3,4-thiadiazol-2-yl]-2,2-dimethylpropanamide;KF 89617;Litronesib;LY 2523355;LY-2523355; KF-89617;Propanamide, N-[4-(2,2-dimethyl-1-oxopropyl)-5-[[[[2-(ethylamino)ethyl]sulfonyl]amino]methyl]-4,5-dihydro-5-phenyl-1,3,4-thiadiazol-2-yl]-2,2-dimethyl-, (5R)-

CAS号:

910634-41-2

分子式:

C23H37N5O4S2

分子量:

511.7

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

910634-41-2.mol

密度 

1.23±0.1 g/cm3(Predicted)

酸度系数(pKa)

9.47±0.40(Predicted)

生物活性

Litronesib (LY2523355) 是一种选择性的有丝分裂特异性运动蛋白 Eg5 抑制剂，具有抗肿瘤的活性。

靶点

Eg5

Eg5

体外研究

Litronesib (LY2523355) is a selective Eg5 inhibitor. Litronesib (25 nM) induces cancer cells to death during mitotic arrest, and this needs sustained activation of spindle-assembly checkpoint (SAC).

体内研究

Litronesib (LY2523355; 1.1, 3.3, 10, and 30 mg/kg, i.v.) shows antitumor activity in a dose-dependently, and causes a dramatic increase in cancer cells immuno-positive for histone H3 phosphorylation in Colo205 xenograft tumors.