PF-04217903 methanesulfonate is a potent ATP-competitive inhibitor of c-Met kinase (Ki of 4.8 nM for human c-Met).

PF-04217903 induces apoptosis of GTL-16 cells (IC50=31 nM) [1]. PF-04217903 methanesulfonate also inhibits HGF-mediated cell migration and Matrigel invasion in several c-Met–overexpressing tumor cell lines such as human NCI-H441 lung carcinoma and HT29 colon carcinoma with IC50 values comparable with those for inhibition of c-Met phosphorylation in these cell lines (IC50= 7-12.5 nM)[1].

PF-04217903 methanesulfonate shows a significant dose-dependent reduction of human IL-8 levels in both the U87MG and GTL-16 models and decreases human VEGFA levels in the GTL-16 model. PF-04217903 methanesulfonate strongly induces phospho-PDGFRβ levels in U87MG xenograft tumors[1].

956906-93-7

C20H20N8O4S

468.49

DMSO:50 mg/mL (106.73 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years