PF-04217903 (phenolsulfonate)

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].

Product Specifications

CAS Number

[1159490-85-3]

UNSPSC

12352005

Target

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 Formula

C25H22N8O5S

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.