Imexon

CAS No. 59643-91-3

Imexon( Amplimexon | BM 06002 )

Catalog No. M15211 CAS No. 59643-91-3

A 2-cyanoaziridine derivative with antitumor activity in some types of cancer.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    Imexon
  • Note
    Research use only, not for human use.
  • Brief Description
    A 2-cyanoaziridine derivative with antitumor activity in some types of cancer.
  • Description
    A 2-cyanoaziridine derivative with antitumor activity in some types of cancer, including pancreatic, lung, breast, prostate, melanoma, and multiple myeloma; induces mitochondrial oxidation and induces apoptosis via a pathway involving cleaved caspase-3, caspase-9, and/or caspase-8; an apoptosis inducer agent.Blood Cancer Phase 2 Clinical.
  • In Vitro
    Imexon (BM 06002) induces oxidative stress in the ER, activates an ER stress response. Imexon (BM 06002) does not significantly alter the levels of eIF2B5, however there is a dose-dependent increase in the phosphorylation of eIF2alpha, as well as an increase in the levels of GTP exchange protein eIF2B2 in MiaPaCa-2, Panc-1, and BxPC3 cells. Imexon (BM 06002) induces single-stranded breaks in the human A375 melanoma cells but only significantly at the highest concentrations for each agent compared to controls. Imexon plus DTIC cytotoxicity is additive. Imexon (BM 06002) show inhibitory activities against MiaPaCa-2, Panc-1 and BxPC3, with IC50s of 275.5 ± 54.2, 147.4 ± 4.7 and 355.7 ± 114.7 μM.
  • In Vivo
    Imexon (BM 06002) in combination with DTIC results in an increase in the peak plasma imexon level in non-tumor-bearing mice. The combination of both drugs increases plasma imexon AUC by 22% (p=0.026). Imexon (BM 06002) (100 mg/kg/day, i.v.) treatment decreases the body weight of SCID mice bearing human A375 melanoma tumors, but there is no significant difference in tumor growth. Imexon (BM 06002) (100 mg/kg) in combination with GEM shows synergistic inhibition of Panc-1 tumor growth in SCID mice.
  • Synonyms
    Amplimexon | BM 06002
  • Pathway
    Apoptosis
  • Target
    Apoptosis
  • Recptor
    Apoptosis
  • Research Area
    Cancer
  • Indication
    Blood cancer

Chemical Information

  • CAS Number
    59643-91-3
  • Formula Weight
    111.104
  • Molecular Formula
    C4H5N3O
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 62.5 mg/mL (562.56 mM)
  • SMILES
    O=C1N2CC2C(N)=N1
  • Chemical Name
    4-Amino-1,3-diazabicyclo[3.1.0]hex-3-en-2-one

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Ziegler AE, et al. Exp Pathol (Jena). 1977;14(6):321-7. 2. Hersh EM, et al. J Natl Cancer Inst. 1992 Aug 19;84(16):1238-44. 3. Baker AF, et al. Clin Cancer Res. 2007 Jun 1;13(11):3388-94.
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