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 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.|
|Incubation time||72 hours|
|Animal models||Mice bearing RT-112, OPM-2 (DSMZ), SNU-16, or NCI-H460 xenograft|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
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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BLU9931 is a potent, selective, and irreversible FGFR4 inhibitor with IC50 of 3 nM, about 297-, 184-, and 50-fold selectivity over FGFR1/2/3, respectively.
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