LY2874455

Catalog No.S7057

For research use only.

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.

LY2874455 Chemical Structure

CAS No. 1254473-64-7

Selleck's LY2874455 has been cited by 10 Publications

1 Customer Review

Purity & Quality Control

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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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-H1581 M{juPWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NE\VVYw4OiCqcoO= NFPXPZJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JGZITlJzLXHtdIxq\mmnZDDoeY1idiCQQ1mtTFE2QDFiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JGNEUzhxTWTUJIF{e2G7LDDJR|UxRDBwMECwOe69VQ>? NW[yRnVTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkezOFg2OzdpPkK3N|Q5PTN5PD;hQi=>
Assay
Methods Test Index PMID
Western blot p-FRS2 / FRS2 / p-AKT / AKT / p-ERK / ERK / p-PLCγ1 / PLCγ1 ; MCL-1 30795553 29408314
Growth inhibition assay Cell death 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 (from reference)

Kinase Assay:

[1]

  • 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]

  • 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).

Animal Research:

[1]

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

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 444.31
Formula

C21H19Cl2N5O2

CAS No. 1254473-64-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C1=C(C=NC=C1Cl)Cl)OC2=CC3=C(C=C2)NN=C3C=CC4=CN(N=C4)CCO

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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