Catalog Number: 5424
Chemical Name: 2-[4-[(2S)-2-(2-Phenyl-1H-benzimidazol-1-yl)-2-(4-piperidinyl)ethoxy]phenyl]-1-(phenylmethyl)-1H-benzimidazole trihydrochloride
Biological Activity
High affinity PDEδ-KRAS interaction inhibitor (Kd = 41 nM); binds to PDEδ. Reduces proliferation and induces cell death of KRAS-dependent Panc-Tu-1 and Capan-1 pancreatic cancer cells. Attenuates tumor growth of Panc-Tu-1 xenografts in mice.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in water and to 100 mM in DMSO
  • Purity:
  • Storage:
    Store at -20°C
  • 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. Small molecule inhibition of the KRAS-PDEδ interaction impairs oncogenic KRAS signalling.
    Zimmermann et al.
    Nature, 2013;497:638
  2. Structure guided design and kinetic analysis of highly potent benzimidazole inhibitors targeting the PDEδ prenyl binding site.
    Zimmermann et al.
    J.Med.Chem., 2014;57:5435
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