Sample solution is provided at 25 µL, 10mM.
|Description||LY2874455 is a potent, selective, small-molecule inhibitor of fibroblast growth factor receptors (FGFR) with IC50 values of 2.8, 2.6, 6.4 and 6 nM for FGFR1, 2, 3, and 4, respectively.|
|IC50||2.8 nM||2.6 nM||6.4 nM||6 nM|
|Cas No.||1254473-64-7||SDF||Download SDF|
|Synonyms||LY 2874455; LY-2874455|
|Solubility||Soluble in DMSO > 10 mM||Storage||Store at -20°C|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
|Shipping Condition||Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
IC50: LY2874455 inhibited the FGF2- and VEGF-induced tube-forming activities, with IC50 values of 0.6 and 3.6 nM, respectively.
The fibroblast growth factor receptors (FGFR) are tyrosine kinases that are present in many types of endothelial and tumor cells and play an important role in tumor cell growth, survival, and migration. LY2874455 is a potent and selective FGFR inhibitor..
In vitro: LY2874455 is active against all four FGFRs. It exhibits a potent activity against FGF/FGFR-mediated signaling in several cancer cell lines. LY2874455 also exhibits a good in vitro selectivity on inhibition of FGF- over VEGF-mediated target signaling .
In vivo: LY2874455 shows an excellent broad spectrum of antitumor activity in several tumor xenograft models representing the major FGF/FGFR relevant tumor histologies, and with a well-defined pharmacokinetic/pharmacodynamic relationship. Furthermore, LY2874455 did not show VEGF receptor 2–mediated toxicities such as hypertension at efficacious doses .
Clinical trial: A Phase 1 study of LY2874455 is to determine the recommended Phase 2 regimen of study drug that may be safely administered to patients with advanced and or metastatic cancer. The study consists of two parts: dose escalation and dose confirmation
 Zhao G, Li WY, Chen D, Henry JR, Li HY, Chen Z, Zia-Ebrahimi M, Bloem L, Zhai Y, Huss K, Peng SB, McCann DJ. A novel, selective inhibitor of fibroblast growth factor receptors that shows a potent broad spectrum of antitumor activity in several tumor xenograft models. Mol Cancer Ther. 2011;10(11):2200-10.