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LY2874455

Cat. No. M3617

LY2874455 Structure
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

LY2874455 is a novel and potent FGF/FGFR inhibitor. LY2874455 exhibits a potent activity against FGF/FGFR-mediated signaling in several cancer cell lines. LY2874455 exhibits a 6- to 9-fold in vitro and in vivo selectivity on inhibition of FGF- over VEGF-mediated target signaling in mice. LY2874455 did not show VEGF receptor 2-mediated toxicities such as hypertension at efficacious doses. Currently, this molecule is being evaluated for its potential use in the clinic.

Protocol
Cell Experiment
Cell lines KMS-11, OPM-2, L-363, U266, SNU-16, KATO-III, NUGC-3 and SH-10-TC cells
Preparation method Growing cells (2,000 per well) first in RPMI for 6 hours and treating with LY2874455 at 37 ℃ for 3 days. Staining the cells at 37℃ for 4 hours and then solubilizing at 37℃ for 1 hour. Finally, using a plate reader (Spectra Max Gemini XS) to read the plate at 570 nm.
Concentrations ~1 μM
Incubation time 72 hours
Animal Experiment
Animal models Mice bearing RT-112, OPM-2 (DSMZ), SNU-16, or NCI-H460 xenograft
Formulation 10% Acacia
Dosages 3 mg/kg
Administration p.o.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 444.31
Formula C21H19Cl2N5O2
CAS Number 1254473-64-7
Purity >99%
Solubility DMSO
Storage at -20°C
References

A novel, selective inhibitor of fibroblast growth factor receptors that shows a potent broad spectrum of antitumor activity in several tumor xenograft models.
Zhao G, et al. Mol Cancer Ther. 2011 Nov;10(11):2200-10. PMID: 21900693.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: LY2874455 supplier, FGFR, inhibitors

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