LY2874455 has been used in trials studying the treatment of Advanced Cancer.

FGFR2:2.6 nM, VEGFR2:7 nM, FGFR3:6.4 nM, FGFR1:2.8 nM, FGFR4:6 nM

In mice carrying xenografts of RT-112, OPM-2 (DSMZ), SNU-16, or NCI-H460, LY2874455 (3 mg/kg, orally administered) demonstrated dose-dependent inhibition of tumor growth. Additionally, LY2874455 effectively inhibited FGF-induced Erk phosphorylation in mouse cardiac tissue, with TED50 and TED90 values of 1.3 and 3.2 mg/kg, respectively.

LY2874455 exhibits FGFR-dependent anti-proliferative effects in KMS-11, OPM-2, SNU-16, and KATO-III cells. In RT-112 cells, HUVECs, KATO-III cells, and SNU-16 cells, LY2874455 inhibits FGF/FGFR-mediated signaling activity.

Biochemical filter-binding assays for detection of FGFR phosphorylation activities : Reaction mixtures contains 8 mM Tris-HCl (pH 7.5), 10 mmol/L HEPES, 5 mM dithiothreitol, 10 μM ATP, 0.5 μCi 33P-ATP, 10 mM MnCl2, 150 mM NaCl, 0.01% Triton X-100, 4% dimethyl sulfoxide, 0.05 mg/mL poly(Glu:Tyr) (4:1, average molecular weight of 20–50 kDa), and 7.5, 7.5, and 16 ng of FGFR1, FGFR3, and FGFR4, respectively, and are incubated at room temperature for 30 minutes followed by termination with 10% H3PO4. The reaction mixtures are transferred to 96-well MAFB filter plates that are washed 3 times with 0.5% H3PO4. After air-drying, the plates are read with a Trilux reader.

Cells (2,000 per well) are first grown in RPMI for 6 hours and treated with LY2874455 at 37 ℃ for 3 days. The cells are stained at 37℃ for 4 hours and then solubilized at 37℃ for 1 hour. Finally, the plate is read at 570 nm using a plate reader (Spectra Max Gemini XS). (Only for Reference)