SSR128129E free acid is an orally available and allosteric inhibitor of FGFR(IC50 of 1.9 μM for FGFR1).

FGFR1:1.9 μM

FGF2-induced EC proliferation(IC50 : 31±1.6 nM) inhibited by SSR128129E, migration with an IC50 of 15.2±4.5 nM, and lamellipodia formation in a dose dependent manner. SSR128129E inhibits responses mediated by FGFR1-4. SSR128129E blocks EC migration in response to FGF1, a ligand of FGFR1 and FGFR4, and capillary tube formation in response to FGF19, a ligand of FGFR4. Proliferation and migration of the murine pancreatic Panc02 tumor cell line in response to FGF7 are also blocked by SSR128129E, showing that SSR128129E inhibits FGFR subtypes of other species as well.

growth of orthotopic Panc02 tumors by 44% and delays growth of Lewis lung carcinomainhibited by Oral delivery of SSR128129E (30 mg/kg/day, from day 3) . oral SSR128129E (30 mg/kg/day, from day 5) reduces tumor size and weight by 53% and 40%, respectively. SSR128129E inhibits the growth of subcutaneous CT26 colon tumors by 34% and of the multidrug resistant MCF7/ADR breast cancer xenograft model by 40%. tumor invasiveness and metastasis of Panc02 tumor cells to peritoneal lymph nodes reduced by SSR128129E .