Molecular Weight(MW): 444.31
LY2874455 is a pan-FGFR inhibitor with IC50 of 2.8 nM, 2.6 nM, 6.4 nM, and 6 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively, and also inhibits VEGFR2 activity with IC50 of 7 nM. Phase 1.
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A: Overall structure of LY2874455/FGFR4 complex. B: The diagram of LY2874455. C: Fo-Fc omit map of LY2874455 in the FGFR4/LY2874455 complex. The electron density is superimposed with the final model. D: The DFG motif conformation of FGFR4. Active ApoFGFR4 DFG-in conformation is shown in blue (PDB: 4QQT); FGFR4/Ponatinib DFG-out conformation is shown in yellow (PDB: 4UXQ); FGFR4/BLU9931 DFG-in conformation is shown in pink (PDB: 4XCU); FGFR4/LY2874455 DFG-in conformation is shown in grey (this work). LY2874455 is highlighted in brown.
PLoS One. 2016, 11(9): e0162491. LY2874455 purchased from Selleck.
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Choose Selective FGFR Inhibitors
|Description||LY2874455 is a pan-FGFR inhibitor with IC50 of 2.8 nM, 2.6 nM, 6.4 nM, and 6 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively, and also inhibits VEGFR2 activity with IC50 of 7 nM. Phase 1.|
In RT-112 cells, HUVECs, KATO-III cells, and SNU-16 cells, LY2874455 inhibits FGF/FGFR-mediated signaling activities. LY2874455 shows FGFR-dependent antiproliferative effects in KMS-11, OPM-2, SNU-16 and KATO-III cells. 
|In vivo||LY2874455 exhibits a potent inhibition of FGF-induced Erk phosphorylation in the heart tissues of mice with TED50 and TED90 values of 1.3 and 3.2 mg/kg, respectively. In mice bearing RT-112, OPM-2 (DSMZ), SNU-16, or NCI-H460 xenograft, LY2874455 (3 mg/kg p.o.) results in dose-dependent inhibition of the tumor growth. |
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.
|In vitro||DMSO||88 mg/mL (198.05 mM)|
|Ethanol||57 mg/mL warmed (128.28 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
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