Catalog Number: 1807
Chemical Name: (17β)-2-Methoxyestra-1,3,5(10)-triene-3,17-diol
Biological Activity
Apoptotic, antiproliferative and antiangiogenic agent, in vitro and in vivo; acts via an estrogen receptor-independent mechanism. Induces p53-induced apoptosis via two pathways: activation of p38 and NF-κB; and activation of JNK and AP-1 leading to Bcl-2 phosphorylation. Also upregulates death receptor 5 and binds to tubulin, inhibiting its assembly.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 50 mM in DMSO
  • Purity:
  • Storage:
    Store at RT
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. 2-Methoxyestradiol, an endogenous mammalian metabolite, inhibits tubulin polymerization by interacting at the colchicine site.
    D'Amato et al.
    Proc.Natl.Acad.Sci.U.S.A., 1994;91:3964
  2. 2-Methoxyestradiol inhibits proliferation and induces apoptosis independently of estrogen receptors α and β.
    LaVallee et al.
    Cancer Res., 2002;62:3691
  3. 2-Methoxyestradiol up-regulates death receptor 5 and induces apoptosis through activation of the extrinsic pathway.
    LaVallee et al.
    Cancer Res., 2003;63:468
  4. Roles of p38 and c-jun NH2-terminal kinase-mediated pathways in 2-methoxyestradiol-induced p53 induction and apoptosis.
    Shimada et al.
    Carcinogenesis, 2003;24:1067
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