Catalog Number: 3567
Chemical Name: 6-(2,6-Dimethylphenyl)-2-[[4-(4-methyl-1-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-one
Biological Activity
Potent inhibitor of lymphocyte specific kinase (Lck). IC50 values are 0.007, 0.021, 0.042 and 0.20 μM for Lck, Lyn, Src and Syk kinases respectively. Displays >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Inhibits T cell proliferation in vitro and inhibits arthritis in two in vivo models. Orally active.
Technical Data
  • M.Wt:
    530.62
  • Formula:
    C31H30N8O
  • Solubility:
    Soluble to 100 mM in DMSO and to 10 mM in ethanol with gentle warming
  • Purity:
    >98%
  • Storage:
    Store at -20°C
  • CAS No:
    847950-09-8
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. Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory
    Martin et al.
    J.Med.Chem., 2008;51:1637

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