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LY2874455

FGF/FGFR Inhibitor

LY2874455

Catalog No. A3576
Size Price Stock Qty
5mg $238.00 In stock
10mg $428.00 In stock
50mg $950.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

LY2874455

Biological Activity

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.
Targets FGFR1 FGFR2 FGFR3 FGFR4    
IC50 2.8 nM 2.6 nM 6.4 nM 6 nM    

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Chemical Properties

Cas No. 1254473-64-7 SDF Download SDF
Synonyms LY 2874455; LY-2874455
Chemical Name 2-[4-[(E)-2-[5-[(1R)-1-(3,5-dichloropyridin-4-yl)ethoxy]-1H-indazol-3-yl]ethenyl]pyrazol-1-yl]ethanol
Canonical SMILES CC(C1=C(C=NC=C1Cl)Cl)OC2=CC3=C(C=C2)NN=C3C=CC4=CN(N=C4)CCO
Formula C21H19Cl2N5O2 M.Wt 444.31
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

Background

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 [1].

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 [1].

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

Reference:
[1] 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.