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.
| 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. |
| Molecular Weight | 444.31 |
| Formula | C21H19Cl2N5O2 |
| CAS Number | 1254473-64-7 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
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