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Chemical Compound Review

Imexonum     4-amino-1,3- diazabicyclo[3.1.0]hex-3-en- 2-one

Synonyms: Amplimexon, Imexon, AGN-PC-004KVF, CHEMBL146428, AG-K-61494, ...
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Disease relevance of Imexon


High impact information on Imexon

  • Imexon reduced the incidence of lymphoma in severe combined immune deficient mice inoculated with human lymphocytes [2].
  • RESULTS: The concentration of imexon that caused 50% inhibition of growth was under 10 micrograms/mL for lymphocytes stimulated with mitogens [2].
  • Cells exposed to inhibitory concentrations of imexon were blocked in cell cycle progression [2].
  • Antiproliferative and antitumor activity of the 2-cyanoaziridine compound imexon on tumor cell lines and fresh tumor cells in vitro [2].
  • Flow cytometric experiments have shown that imexon treatment is associated with the formation of reactive oxygen species (ROS) and the loss of mitochondrial membrane potential (Deltapsi(m)) in imexon-sensitive myeloma cell lines and NB-4 cells [3].

Biological context of Imexon


Anatomical context of Imexon


Associations of Imexon with other chemical compounds


Gene context of Imexon

  • Although there was a positive correlation between increasing CuZnSOD levels and imexon resistance, no relationship was found for catalase, Bcl-2, mitochondrial thioredoxin or MnSOD levels [10].
  • Imexon cytotoxicity was unchanged in three RPMI8226 cell lines with different levels (low, medium and high) of FAS expression [11].
  • However, it was unknown whether imexon activates an intrinsic apoptotic pathway that is associated with activation of caspase-9 or an extrinsic pathway that is induced by receptor-mediated signals such as Fas ligand characterized by caspase-8 activation [11].
  • Damage to mitochondrial DNA was detected by a semiquantitative polymerase chain reaction assay in imexon-treated RPMI 8226 cells; however, nuclear DNA was not affected [3].
  • The following immunomodulators were evaluated, listed in the order of their ability to inhibit the FV disease: imexon > MVE-2 > human recombinant IFN-alpha A/D > AS101 > ampligen > AM-3 = oxamisole > ImuVert > bropirimine [12].

Analytical, diagnostic and therapeutic context of Imexon


  1. Sensitivity of multiple myeloma to imexon in the human tumor cloning assay. Salmon, S.E., Hersh, E.M. J. Natl. Cancer Inst. (1994) [Pubmed]
  2. Antiproliferative and antitumor activity of the 2-cyanoaziridine compound imexon on tumor cell lines and fresh tumor cells in vitro. Hersh, E.M., Gschwind, C.R., Taylor, C.W., Dorr, R.T., Taetle, R., Salmon, S.E. J. Natl. Cancer Inst. (1992) [Pubmed]
  3. Induction of mitochondrial changes in myeloma cells by imexon. Dvorakova, K., Waltmire, C.N., Payne, C.M., Tome, M.E., Briehl, M.M., Dorr, R.T. Blood (2001) [Pubmed]
  4. Preclinical pharmacokinetics and antitumor activity of imexon. Dorr, R.T., Liddil, J.D., Klein, M.K., Hersh, E.M. Investigational new drugs. (1995) [Pubmed]
  5. Imexon-induced apoptosis in multiple myeloma tumor cells is caspase-8 dependent. Evens, A.M., Prachand, S., Shi, B., Paniaqua, M., Gordon, L.I., Gartenhaus, R.B. Clin. Cancer Res. (2004) [Pubmed]
  6. Preclinical antitumor activity, pharmacokinetics and pharmacodynamics of imexon in mice. Pourpak, A., Meyers, R.O., Samulitis, B.K., Sherry Chow, H.H., Kepler, C.Y., Raymond, M.A., Hersh, E., Dorr, R.T. Anticancer Drugs (2006) [Pubmed]
  7. Suppression of human lymphoma development in the severe combined immune-deficient mouse by imexon therapy. Hersh, E.M., Grogan, T.M., Funk, C.Y., Taylor, C.W. J. Immunother. (1993) [Pubmed]
  8. Effect of imexon treatment on Friend virus complex infection using genetically defined mice as a model for HIV-1 infection. Morrey, J.D., Warren, R.P., Okleberry, K.M., Burger, R.A., Chirigos, M.A., Sidwell, R.W. Antiviral Res. (1991) [Pubmed]
  9. Induction of oxidative stress and apoptosis in myeloma cells by the aziridine-containing agent imexon. Dvorakova, K., Payne, C.M., Tome, M.E., Briehl, M.M., McClure, T., Dorr, R.T. Biochem. Pharmacol. (2000) [Pubmed]
  10. Correlates of imexon sensitivity in human multiple myeloma cell lines. Samulitis, B.K., Landowski, T.H., Dorr, R.T. Leuk. Lymphoma (2006) [Pubmed]
  11. Imexon activates an intrinsic apoptosis pathway in RPMI8226 myeloma cells. Dvorakova, K., Payne, C.M., Landowski, T.H., Tome, M.E., Halperin, D.S., Dorr, R.T. Anticancer Drugs (2002) [Pubmed]
  12. Immunomodulator effects on the Friend virus infection in genetically defined mice. Sidwell, R.W., Morrey, J.D., Okleberry, K.M., Burger, R.A., Warren, R.P. Ann. N. Y. Acad. Sci. (1993) [Pubmed]
  13. Treatment of the murine, retrovirus-induced lymphoproliferative immunodeficiency disease (LP-BM5) in C57BL/10 mice with the immunomodulator Imexon. Funk, C.Y., Eisman, J., Hersh, E.M. AIDS Res. Hum. Retroviruses (1992) [Pubmed]
  14. Pharmaceutical development of a lyophilised dosage form for the investigational anticancer agent Imexon using dimethyl sulfoxide as solubilising and stabilising agent. den Brok, M.W., Nuijen, B., Lutz, C., Opitz, H.G., Beijnen, J.H. Journal of pharmaceutical sciences. (2005) [Pubmed]
  15. Imexon-based combination chemotherapy in A375 human melanoma and RPMI 8226 human myeloma cell lines. Scott, J., Dorr, R.T., Samulitis, B., Landowski, T.H. Cancer Chemother. Pharmacol. (2007) [Pubmed]
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