PF-04217903 (phenolsulfonate)

• UNSPSC Description:

  PF-04217903 phenolsulfonate is a potent ATP-competitive c-Met kinase inhibitor with Ki of 4.8 nM for human c-Met. PF-04217903 phenolsulfonate shows more than 1,000-fold selectivity relative to 208 kinases. Antiangiogenic properties[1][2].

• Target Antigen:

  c-Met/HGFR

• Type:

  Reference compound

• Related Pathways:

  Protein Tyrosine Kinase/RTK

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/pf-04217903-phenolsulfonate.html

• Solubility:

  10 mM in DMSO

• Smiles:

  O=S(C1=CC=C(O)C=C1)(O)=O.OCCN2N=CC(C3=CN=C4C(N(CC5=CC=C6N=CC=CC6=C5)N=N4)=N3)=C2

• Molecular Weight:

  546.56

• References & Citations:

  [1]Zou HY, et al. Sensitivity of selected human tumor models to PF-04217903, a novel selective c-Met kinase inhibitor. Mol Cancer Ther. 2012 Apr;11(4):1036-47.|[2]Cui JJ, et al. 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-yl)-1H-pyrazol-1-yl)ethanol (PF-04217903) for the treatment of cancer. J Med Chem. 2012 Sep 27;55(18):8091-109.|[3]Timofeevski SL, et al. Enzymatic characterization of c-Met receptor tyrosine kinase oncogenic mutants and kinetic studies with aminopyridine and triazolopyrazine inhibitors. Biochemistry. 2009 Jun 16;48(23):5339-49.

• Shipping Conditions:

  Room temperature

• Clinical Information:

  Phase 1

• CAS Number:

  1159490-85-3