LY2874455

For research use only.

Catalog No.S7057

6 publications

LY2874455 Chemical Structure

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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Selleck's LY2874455 has been cited by 6 publications

1 Customer Review

  • 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.

Purity & Quality Control

Choose Selective FGFR Inhibitors

Biological Activity

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.
Targets
FGFR2 [1]
(Cell-free assay)		 FGFR1 [1]
(Cell-free assay)		 FGFR4 [1]
(Cell-free assay)		 FGFR3 [1]
(Cell-free assay)		 VEGFR2 [1]
(Cell-free assay)
2.6 nM 2.8 nM 6 nM 6.4 nM 7 nM
In vitro

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. [1]
Assay
Methods Test Index PMID
Western blot
p-FRS2 / FRS2 / p-AKT / AKT / p-ERK / ERK / p-PLCγ1 / PLCγ1 ; 

PubMed: 30795553     


The level of phosphorylated and total protein for the indicated proteins in NRH-LS1, LPS510 and LPS853 cells treated for 24 h with 100 nM of LY2874455, with or without FGF as indicated. In all Western blot experiments α-tubulin was used as a loading control.

MCL-1; 

PubMed: 29408314     


After KMCH and KMBC cells were treated with increasing concentrations of LY2874455 (LY) for 24 h, MCL1 mRNA and mitochondrial protein levels were assessed by qPCR and western blotting, respectively. HSP60 was used as a loading control for mitochondrial lysate.

30795553 29408314
Growth inhibition assay
Cell death ; 

PubMed: 29408314     


Cell death rate of KMCH and KMBC cells assessed by MTS and SRB assay after a 24 h treatment with LY (5 μM).

29408314
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. [1]

Protocol

Kinase Assay:

[1]
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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.
Cell Research:

[1]
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  • Cell lines: KMS-11, OPM-2, L-363, U266, SNU-16, KATO-III, NUGC-3 and SH-10-TC cells
  • Concentrations: ~1 μM
  • Incubation Time: 72 hours
  • Method:

    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)
Animal Research:

[1]
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  • Animal Models: Mice bearing RT-112, OPM-2 (DSMZ), SNU-16, or NCI-H460 xenograft
  • Dosages: 3 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 88 mg/mL (198.05 mM)
Ethanol 57 mg/mL warmed (128.28 mM)
Water Insoluble
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. 		5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 444.31
Formula

C21H19Cl2N5O2
CAS No. 1254473-64-7
Storage powder
in solvent
Synonyms N/A
Smiles CC(C1=C(C=NC=C1Cl)Cl)OC2=CC3=C(C=C2)NN=C3C=CC4=CN(N=C4)CCO

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03125239 Completed Drug: Merestinib|Drug: LY2874455 Relapsed Adult Acute Myeloid Leukemia|Refractory Adult Acute Myeloid Leukemia Jacqueline Garcia MD|Eli Lilly and Company|Dana-Farber Cancer Institute August 10 2017 Phase 1
NCT01212107 Completed Drug: FGF Receptor|Drug: Phosphate Binders Advanced Cancer Eli Lilly and Company December 2010 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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FGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID