2375740-98-8
中文名称
化合物 T10895
英文名称
1H-Pyrazole-5-carboxamide, 3-(difluoromethyl)-1-(1-methylethyl)-N-[6-[(5S,6S)-6,7,8,9-tetrahydro-6-hydroxy-5H-imidazo[1,5-a]azepin-5-yl][1,1'-biphenyl]-3-yl]-
CAS
2375740-98-8
分子式
C28H29F2N5O2
分子量
505.56
MOL 文件
2375740-98-8.mol
2375740-98-8 结构式
基本信息
中文别名
化合物 T10895 英文别名
1H-Pyrazole-5-carboxamide, 3-(difluoromethyl)-1-(1-methylethyl)-N-[6-[(5S,6S)-6,7,8,9-tetrahydro-6-hydroxy-5H-imidazo[1,5-a]azepin-5-yl][1,1'-biphenyl]-3-yl]-物理化学性质
沸点666.5±55.0 °C(Predicted)
密度1.35±0.1 g/cm3(Predicted)
储存条件Store at -20°C, protect from light, stored under nitrogen
溶解度DMSO:50.56(Max Conc. mg/mL);100.0(Max Conc. mM)
酸度系数(pKa)12.66±0.70(Predicted)
形态Solid
颜色Light yellow to yellow
常见问题列表
生物活性
CSN5i-3 是一种有效的，选择性和口服的 CSN5/Jab1 抑制剂，抑制 CSN 催化的 Cul1 deneddylation IC50 值为 5.8 nM。靶点
IC50: 5.8 nM (CSN5)
体外研究
CSN5i-3 traps CRLs in the neddylated state, which leads to inactivation of a subset of CRLs by inducing degradation of their substrate recognition module.
体内研究
CSN5i-3 shows a good pharmacokinetic profile. CSN5i-3 inhibits growth of human xenograft. Treatment with CSN5i-3 triggers the formation of cleaved PARP and cleaved caspase 3 indicative of apoptosis induction.