Nutlin-3a chiral

- Overview
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    Background
    
    Nutlin-3 is a small-molecule inhibitor of MDM2 (mouse double minute 2) with IC50 value of 0.09μM [1].
    Nutlin-3 binds MDM2 in the TP53-bindingpocket, thereby interfering with MDM2-directed TP53 degradation. This has been shown to cause cell cycle arrest, growth inhibitionand apoptosis in both solid tumors and lymphoid neoplasms.In mantle cell lymphoma(MCL), it is reported that Nutlin-3 can inhibit cell growth and activate apoptosis in bothwt-TP53(IC50 of 1 to 10μM) and mt-TP53(IC50 of 22.5μM) cells [2].
    Nutlin-3 can also effectcell cycle in gastric cancer cell lines. It induces G1 arrest inMKN-45 and SNU-1 cell lines. In vitro assay shows Nutlin-3can enhance the antitumoreffects of conventional chemotherapeutic agents in several gastric cancer cell lines. And in in vivo assay, Nutlin-3 significantly inhibits the growth of xenograft tumors [3].
    
    [1] Lyubomir T.Vassilev et al. In vivo activation of the p53 pathway by small-molecule antagonists of MDM2.Science.2004, 303: 844-848.
    [2] Yoko Tabe, Denise Sebasigari, Linhua Jin, et al.MDM2 Antagonist Nutlin-3 Displays Antiproliferative andProapoptotic Activity in Mantle Cell Lymphoma. Clin Cancer Res. 2009, 15:933-942.
    [3] Shinji Endo,Kenji Yamato,Sachiko Hirai,Toshikazu Moriwaki,Kuniaki Fukuda,Hideo Suzuki,Masato Abei,Ichiro Nakagawa and IchinosukeHyodo.Potent in vitro and in vivo antitumor effects ofMDM2 inhibitor nutlin-3 in gastric cancer cells.Cancer Science. 2011, 102 (3): 605-613.
- Properties
  - Alternative Name
    
    Nutlin-3a;Nutlin 3a; 4-[(4S,5R)-4,5-bis(4-chlorophenyl)-2-(4-methoxy-2-propan-2-yloxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazin-2-one
    
    CAS Number
    
    675576-98-4
    
    Molecular Formula
    
    C30H30Cl2N4O4
    
    Molecular Weight
    
    581.49
    
    Appearance
    
    A solid
    
    Purity
    
    97.11%
    
    Solubility
    
    ≥29.07 mg/mL in DMSO; insoluble in H2O; ≥104.4 mg/mL in EtOH
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Xinzhi Yang, Jiangang Liu, et al. "miR-18a promotes glioblastoma development by down-regulating ALOXE3-mediated ferroptotic and anti-migration activities." Oncogenesis. 2021 Feb 12;10(2):15. PMID:33579899
    2. Roscoe I, Parker M, et al. "Human Serum Albumin and the p53-Derived Peptide Fusion Protein Promotes Cytotoxicity Irrespective of p53 Status in Cancer Cells." Mol Pharm. 2018 Oct 10. PMID:30226785
    3. Chen R, Zhou J, et al. "A Fusion Protein of the p53 Transaction Domain and the p53-Binding Domain of the Oncoprotein MdmX as an Efficient System for High-Throughput Screening of MdmX Inhibitors." Biochemistry. 2017 Jun 27;56(25):3273-3282. PMID:28581721

Nutlin-3a chiral

Background

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