910634-41-2
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
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
CAS
910634-41-2
分子式
C23H37N5O4S2
分子量
511.7
MOL 文件
910634-41-2.mol
910634-41-2 结构式
基本信息
中文别名
EG5变构抑制剂(LITRONESIB)(-)-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
英文别名
KF 89617LY 2523355
Litronesib
LY-2523355
KF-89617
(-)-N-[4-(2,2-Dimethylpropanoyl)-5-[[2-(ethylamino)ethanesulfonamido]methyl]-5-phenyl-4,5-dihydro-1,3,4-thiadiazol-2-yl]-2,2-dimethylpropanamide
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)-
物理化学性质
密度1.23±0.1 g/cm3(Predicted)
储存条件-20°C储存
溶解度DMSO : ≥ 50 mg/mL (97.71 mM)
酸度系数(pKa)9.47±0.40(Predicted)
形态Solid
颜色White to off-white
常见问题列表
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
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Eg5
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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.