Catalog Number: 4239
Chemical Name: 4-[1-(6-Quinolinylmethyl)-1H-1,2,3-triazolo[4,5-b]pyrazin-6-yl]-1H-pyrazole-1-ethanol mesylate
Biological Activity
Highly selective, high affinity MET inhibitor (Ki = 6-7 nM against wild type c-Met). Displays >1000-fold selectivity for c-Met over a panel of 208 kinases.
Technical Data
  • M.Wt:
    468.49
  • Formula:
    C19H16N8O.CH3SO3H
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at +4°C
  • CAS No:
    956906-93-7
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.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from Pfizer Inc.
Background References
  1. Novel therapeutic inhibitors of the c-Met signaling pathway in cancer.
    Eder et al.
    Clin.Cancer Res., 2009;15:2207
  2. Enzymatic characterization of c-Met receptor tyrosine kinase oncogenic mutants and kinetic studies with aminopyridine and triazolopyrazine inhibitors.
    Timofeevski et al.
    Biochemistry, 2009;48:5339
  3. Discovery of small molecule c-Met inhibitors: evolution and profiles of clinical candidates.
    Underiner et al.
    Anticancer Agents Med.Chem., 2010;10:7
  4. Discovery of a novel class of exquisitely selective mesenchymal-epithelial transition factor (c-MET) protein kinase inhibitors and identification of the clinical candidate 2-(4-(1-(quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-
    Cui et al.
    J.Med.Chem., 2012;55:8091
Citations:

The citations listed below are publications that use Tocris products. Selected citations for PF 04217903 mesylate include:

1 Citations: Showing 1 - 1

  1. CD44 plays a functional role in Helicobacter pylori-induced epithelial cell proliferation.
    Authors: Bertaux-Skeirik Et al.
    PLoS Pathog 2015;11:e1004663

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