Name: Apogossypolone (ApoG2)
Price: 840.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    Apogossypolone is an inhibitor of Bcl-2, Mcl-1 and Bcl-XL with Ki values of 35nM, 25nM and 660nM, respectively [1].The MTT-based cell cytotoxicity assay shows that apogossypolone has an anticancer activity with IC50 values of 1, 2 and 3μM, respectively in PC-3, DU-145 (human prostate cancer cell lines) and MDA-MB-231(human breast cancer cell line). Apogossypolone is also found to inhibit the colony formation of DU-145 cells. The mechanism is that apogossypolone binds to Bcl-2 and prevents its association with BH3-only pro-apoptotic proteins, leading the pro-apoptotic proteins to participate in the apoptotic response [2].Besides prostate cancer and breast cancer, apogossypolone is also potent in follicular lymphoma. Apogossypolone significantly inhibits the cell growth via inducing apoptosis in WSU-FSCCL cell line with IC50 value of 109.2nM at 72h [3].
    
    [1] Zhang XQ, Huang XF, Hu XB, Zhan YH, An QX, Yang SM, Xia AJ, Yi J, Chen R, Mu SJ, Wu DC. Apogossypolone, a novel inhibitor of antiapoptotic Bcl-2 family proteins, induces autophagy of PC-3 and LNCaP prostate cancer cells in vitro. Asian J Androl. 2010 Sep;12(5):697-708.
    [2] Zhan Y, Jia G, Wu D, Xu Y, Xu L. Design and synthesis of a gossypol derivative with improved antitumor activities. Arch Pharm (Weinheim). 2009 Apr;342(4):223-9.
    [3] Arnold AA, Aboukameel A, Chen J, Yang D, Wang S, Al-Katib A, Mohammad RM. Preclinical studies of Apogossypolone: a new nonpeptidic pan small-molecule inhibitor of Bcl-2, Bcl-XL and Mcl-1 proteins in Follicular Small Cleaved Cell Lymphoma model. Mol Cancer. 2008 Feb 14;7:20.
- Properties
  - Alternative Name
    
    6,6',7,7'-tetrahydroxy-5,5'-diisopropyl-3,3'-dimethyl-[2,2'-binaphthalene]-1,1',4,4'-tetraone
    
    CAS Number
    
    886578-07-0
    
    Molecular Formula
    
    C28H26O8
    
    Molecular Weight
    
    490.5
    
    Appearance
    
    A solid
    
    Purity
    
    98.50%
    
    Solubility
    
    ≥24.55 mg/mL in DMSO; insoluble in H2O; ≥51.2 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Lin D, Wang X, et al. "Apogossypolone acts as a metastasis inhibitor via up-regulation of E-cadherin dependent on the GSK-3/AKT complex." Am J Transl Res. 2019 Jan 15;11(1):218-232. PMID:30787981
    2. Lin D, Li X, et al. "Apogossypolone (ApoG2) induces ROS-dependent apoptosis and reduces invasiveness of PC12 cells in vitro and in vivo." Am J Transl Res. 2017 Sep 15;9(9):3990-4002. eCollection 2017. PMID:28979675

Apogossypolone (ApoG2)

Apogossypolone (ApoG2)

Background

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