LY-2874455 Inhibitor CAS No. 1254473-64-7

Cat. No.	Name	Size	Price
KI2833	LY-2874455	5 mg	$728
	LY-2874455	10 mg	$1248
	LY-2874455	20 mg	$2028
	LY-2874455	50 mg	$2860
	LY-2874455	100 mg	$4160
	LY-2874455	200 mg	$5980
	LY-2874455	1 g	$14300

Chemical Characteristic

Product Name	LY-2874455
CAS No.	1254473-64-7
Molecular Weight	444.32
Formula	C₂₁H₁₉Cl₂N₅O₂
Chemical Name	2-[4-[(E)-2-[5-[(1R)-1-(3,5-dichloropyridin-4-yl)ethoxy]-1H-indazol-3-yl]ethenyl]pyrazol-1-yl]ethanol
Smiles	C(Cn1ncc(c1)/C=C/c1n[nH]c2c1cc(cc2)O[C@H](C)c1c(cncc1Cl)Cl)O
Chemical Structure

Biological activities

LY2874455 is a potent FGF/FGFR inhibitor. LY2874455 inhibits FGFR1, 2, 3, and 4 in a dose-dependent manner, with IC50 values of 2.8, 2.6, 6.4, and 6 nM, respectively. In addition, LY2874455 inhibits VEGFR2 with an IC50 of 7 nM. In vitro, the IC50s of LY2874455 for KMS-11, OPM-2, L-363, and U266 cells are 0.57, 1.0, 60.4, and 290.7 nM, respectively. In addition, LY2874455 is significantly more potent (6-fold) at inhibiting the tube-forming activity induced by FGF2 than VEGF in vitro. In several cancer cell lines with altered FGFR or FGF levels, RT-112 (overexpressing FGFR3), SNU-16 (amplified FGFR2), OPM-2 (overexpressing a mutant FGFR3 because of a chromosomal translocation), and NCI-H460 (a high level of FGF2) established tumor xenograft models, LY2874455 exhibits rapid, robust, dose-dependent inhibition of tumor growth in vivo.^[1]

References

[1] Zhao G, et al. 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): 2200-2210.

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