货号 | 17003-50mg |
描述 | Mouse double minute 2 protein (Mdm2) is an E3 ubiquitin-protein ligase that binds and ubiquitinates the tumor suppressor p53, leading to its degradation by the proteasome.1 SP 141 is a cell-permeable inhibitor of Mdm2 (Ki = 28 nM).2 Binding of Mdm2 by SP 141 promotes its auto-ubiquitination and proteasomal degradation.2,3 SP 141 induces cell cycle arrest and apoptosis in breast and pancreatic cancer cell lines and inhibits xenograft tumor growth in vivo.2,3 This compound has a short half-life in plasma and wide tissue distribution in tumor-bearing nude mice.4 |
别名 | AGN-PC-0D106I; |
供应商 | Cayman |
应用文献 | |
1.Vassilev, L.T.,Vu, B.T.,Graves, B., et al. In vivo activation of the p53 pathway by small-molecule antagonists of MDM2. Science 303, 844-848 (2004). 2.Wang, W.,Qin, J.J.,Voruganti, S., et al. The pyrido[b]indole MDM2 inhibitor SP-141 exerts potent therapeutic effects in breast cancer models. Nat.Commun. 5, 1-12 (2014). 3.Wang, W.,Qin, J.J.,Voruganti, S., et al. Identification of a new class of MDM2 inhibitor that inhibits growth of orthotopic pancreatic tumors in mice. Gastroenterology 147(4), 893-902 (2014). 4.Nag, S.,Qin, J.J.,Voruganti, S., et al. Development and validation of a rapid HPLC method for quantitation of SP-141, a novel pyrido[b]indole anticancer agent, and an initial pharmacokinetic study in mice. Biomedical Chromatography 29(5), 654-663 (2015). | |
运输条件 | Wet ice in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 324.4 |
分子式 | C22H16N2O |
CAS号 | 1253491-42-7 |
稳定性 | ≥ 2 years |
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