SP-141 是一种 Mdm2 抑制剂,可促进 Mdm2 自身泛素化和降解,具有抗癌活性。
产品描述
SP 141 is a MDM2 inhibitor.SP-141 promotes MDM2 auto-ubiquitination and degradation, with anticancer activity.
体外活性
SP141, which bound directly to MDM2, promoting its auto-ubiquitination and degradation by the proteasome.?The compound reduced levels of MDM2 in pancreatic cancer cell lines, as well as their proliferation, with 50% inhibitory concentrations<0.5 μM (0.38-0.50 μM).?Increasing concentrations of SP141 induced increasing levels of apoptosis and G2-M-phase arrest of pancreatic cancer cell lines, whether or not they expressed functional P53[1].
体内活性
Injection of nude mice with SP141 (40 mg/kg/d) inhibited growth of xenograft tumors (by 75% compared with control mice), and led to regression of orthotopic tumors[1].
Cas No.
1253491-42-7
分子式
C22H16N2O
分子量
324.383
别名
SP 141
储存和溶解度
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years