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| Product Name: | SP 141 | | Synonyms: | SP 141;6-methoxy-1-(naphthalen-1-yl)-9H-pyrido[3,4-b]indole;9H-Pyrido[3,4-b]indole, 6-methoxy-1-(1-naphthalenyl)-;SP 141;SP141;;6-Methoxy-1-(1-naphthalenyl)-9H-pyrido[3,4-b]indole;6-Methoxy-1-(1-naphthyl)-9H-β-carboline;pancreatic,SP-141,inhibit,Inhibitor,cancer,MDM-2/p53,breast,degradation,auto-ubiquitination,SP141 | | CAS: | 1253491-42-7 | | MF: | C22H16N2O | | MW: | 324.38 | | EINECS: | | | Product Categories: | API | | Mol File: | 1253491-42-7.mol |  |
| | SP 141 Chemical Properties |
| Boiling point | 571.2±45.0 °C(Predicted) | | density | 1.284±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | ≤100mg/ml in ethanol;30mg/ml in DMSO;50mg/ml in dimethyl formamide | | form | crystalline solid | | pka | 15.04±0.40(Predicted) | | color | White to yellow |
| | SP 141 Usage And Synthesis |
| Description | 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. SP 141 is a cell-permeable inhibitor of MDM2 (Ki = 28 nM). Binding of MDM2 by SP 141 promotes its auto-ubiquitination and proteasomal degradation. SP 141 induces cell cycle arrest and apoptosis in breast and pancreatic cancer cell lines and inhibits xenograft tumor growth in vivo. This compound has a short half-life in plasma and wide tissue distribution in tumor-bearing nude mice. | | Uses | SP 141 induces cell cycle arrest and apoptosis in breast and pancreatic cancer cell lines, inhibiting xenograft tumor growth in vivo. | | storage | Store at +4°C | | references | [1]. vassilev lt, vu bt, graves b, et al. in vivo activation of the p53 pathway by small-molecule antagonists of mdm2. science. 2004 feb 6;303(5659):844-8.
[2]. wang w, qin jj, voruganti s, et al. the pyrido[b]indole mdm2 inhibitor sp-141 exerts potent therapeutic effects in breast cancer models. nat commun. 2014 oct 1;5:5086.
[3]. wang w, qin jj, voruganti s, et al. identification of a new class of mdm2 inhibitor that inhibits growth of orthotopic pancreatic tumors in mice. gastroenterology. 2014 oct;147(4):893-902.e2.
[4]. nag s, qin jj, 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. biomed chromatogr. 2015 may;29(5):654-63. |
| | SP 141 Preparation Products And Raw materials |
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